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Tocris社
Pfizer社 ライセンス化合物

Tocris社では、製薬会社と試薬研究用途として取扱い契約した化合物を販売しています。
ファイザー社のライセンス化合物をご紹介いたします。


コードNo. メーカーコード 品名 容量 希望納入価格
製品概要 構造式
化学名
CAS No. 分子式=分子量
保存温度 含量 溶解性
512-86071 3776/10 Atorvastatin hemicalcium salt 10mg
- 3776/50 50mg
Potent HMG-CoA reductase inhibitor (IC50 = 8 nM). Reduces circulating LDL-C by inhibiting cholesterol biosynthesis and inducing expression of LDL receptors. Inhibits smooth muscle cell proliferation in vitro and exhibits antinociceptive effects in the inflammatory hypernociception model. atorvastatin-hemicalcium-salt_3776.png
(R,R)-2-(4-Fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemicalcium salt
134523-03-8 C33H34FN2O5.1/2Ca=577.67
4℃ ≧99%(HPLC) 100 mM in DMSO
512-92181 4350/10 Axitinib 10mg
- 4350/50 50mg
Potent inhibitor of VEGFR-2, -3, and -1 (IC50 values are 0.2, 0.1-0.3, and 1.2 nM respectively). Exhibits minimal activity against a panel of 〜100 protein kinase. Inhibits angiogenesis and vascular permeability. Also a high affinity BCR-ABL1 (T315I) inhibitor (Ki = 149 pM for autophosphorylated ABL1 (T315I)). Blocks proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Orally available.

axitinib_4350.png

N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide
319460-85-0 C22H18N4OS=386.47
4℃ ≧99%(HPLC) 25 mM in DMSO
515-86061 3771/50 Azithromycin 50mg
Macrolide antibiotic. Inhibits 50S ribosomal subunit formation and elongation at transpeptidation step in gram-positive and gram-negative organisms. Orally active with improved pharmacokinetics over erythromycin in mouse models. Inhibits autophagy.

azithromycin_3771.png

13-[(2,6-Dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one
83905-01-5 C38H72N2O12=748.98
-20℃ ≧99%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5263/10 Bazedoxifene acetate 10mg
- 5263/50 50mg
Potent selective estrogen receptor modulator (SERM) (IC50 values are 26 and 99 nM for Erα and Erβ respectively). Inhibits 17β-estradiol-induced proliferation in MCF-7 cells. Co-treatment with Raloxifene (Cat No. 2280) completely abolishes raloxifene-induced stimulation of luminal epithelial cells and myometrium.

bazedoxifene-acetate_5263.png

1-[[4-[2-(Hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate
198481-33-3 C30H34N2O3.C2H4O2=530.65
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
517-90171 4283/10 Begacestat 10mg
- 4283/50 50mg
γ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). Orally active. begacestat_4283.png
5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide
769169-27-9 C9H8ClF6NO3S2=391.74
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 4361/10 Bosutinib 10mg
- 4361/50 50mg
Dual inhibitor of Abl and Src kinases (IC50 = 1.2 nM for Src in an enzymatic assay). Displays antiproliferative activity against chronic myelogenous leukemia (CML) cells and decreases the motility and invasion of breast cancer cell lines. Also exhibits potent antiproliferative activity in anchorage-independent, Src-transformed rat fibroblasts (IC50 = 100 nM). Displays selectivity for Src over non-Src family kinases such as growth factor receptor tyrosine kinases.

bosutinib_4361.png

4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
380843-75-4 C26H29Cl2N5O3=530.45
4℃ ≧99%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
- 5916/5 Canertinib dihydrochloride 5mg
- 5916/25 25mg
Potent EGFR kinase inhibitor (IC50 = 7.4 nM). Blocks autophosphorylation of erbB2. Inhibits growth of A431 tumor xenografts in mice. Cell permeable.

canertinib-dihydrochloride_5916.png

N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride
289499-45-2 C24H25ClFN5O3.2HCl=558.86
-20℃ ≧98%(HPLC) 20 mM in water and to 100 mM in DMSO
554-21771 4420/10 Carbazeran citrate 10mg
- 4420/50 50mg
Aldehyde oxidase (AO) substrate. Exhibits activities as a phosphodiesterase inhibitor; produces concentration-dependent positive inotropic responses in isolated right atria.

carbazeran-citrate_4420.png

Ethyl 1-(6,7-dimethoxy-1-phthalazinyl)-4-piperidinyl carbamate citrate
153473-94-0 C18H24N4O4.C6H8O7=552.53
4℃ ≧98%(HPLC) 50 mM in water and to 100 mM in DMSO
516-86091 3786/10 Celecoxib 10mg
- 3786/50 50mg
Selective cyclooxygenase-2 (COX-2) inhibitor (IC50 values are 15 and 0.04 µM for COX-1 and COX-2 respectively). Anti-inflammatory with shorter plasma half-life in vivo than SC 58121 (Cat. No. 2895). Displays chemopreventive activity in in vivo tumor models.

celecoxib_3786.png

4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonamide
169590-42-5 C17H14F3N3O2S=381.37
RT ≧99%(HPLC) 25 mM in DMSO and to 50 mM in ethanol
- 2942/1 CI 1020 1mg
- 2942/10 10mg
- 2942/50 50mg
Highly selective, orally active, non-peptide endothelin-A receptor (ETA) antagonist (IC50 values are 0.3 and 480 nM for ETA and ETB receptors respectively). Antihypertensive; blocks ET-1-induced pressor responses following oral administration.

ci-1020_2942.png

3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]-2(5H)-furanone
162256-50-0 C28H26O9=506.5
-20℃ ≧98%(HPLC) 50 mM in DMSO
551-21801 4822/10 Clindamycin hydrochloride 10mg
- 4822/50 50mg
Lincosamide antibiotic. Inhibits protein synthesis by binding to the 50S ribosomal subunit and preventing early peptide chain elongation in bacteria.

clindamycin-hydrochloride_4822.png

Methyl-7-chloro-6,7,8-trideoxy-6-[[[(2S,4R)-1-methyl-4-propyl-2-pyrrolidinyl]carbonyl]amino]-1-thio-L-threo-α-D-galacto-octopyranoside hydrochloride
21462-39-5 C18H33ClN2O5S.HCl=461.44
-20℃ ≧98%(HPLC) 100 mM in DMSO
515-91711 4193/10 CP 100356 hydrochloride 10mg
- 4193/50 50mg
High affinity P-glycoprotein (P-gp) inhibitor (Ki values are 58 and 94 nM for mouse Pgp1a and Pgp1b isoforms). Inhibits calcein-AM uptake in MDR1-transfected MDCKII cells (IC50 = 0.5 µM) and prazosin transport in BCRP-transfected MDCKII cells (IC50 = 1.5 µM). Displays weak or no inhibitory activity against MRP1, OATP1B1 and several major human P450 enzymes (IC50 > 50 µM).

cp-100356-hydrochloride_4193.png

4-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-N-2[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxy-2-quinazolinamine hydrochloride
142715-48-8 C31H36N4O6.HCl=597.1
RT ≧98%(HPLC) 20 mM in DMSO
513-94291 3783/10 CP 135807 10mg
- 3783/50 50mg
Selective 5-HT1D receptor agonist. Produces dose-dependent decreases in extracellular 5-HT concentration. cp-135807_3783.png
3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-N-(3-nitro-2-pyridinyl)-1H-indol-5-amine
151272-90-1 C19H21N5O2=351.4
4℃ ≧98%(HPLC) 100 mM in DMSO
519-56171 2779/10 CP 154526 10mg
- 2779/50 50mg
Selective, non-peptide CRF1 receptor antagonist (Ki values are 2.7 and > 10000 nM for CRF1 and CRF2 receptors respectively). Blocks CRF-induced adenylate cyclase activation (Ki = 3.7 nM) and attenuates activation of the HPA axis by CRF. Displays anxiolytic-like activity in the rat elevated plus-maze test; brain penetrant. cp-154526_2779.png
N-Butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride
257639-98-8 C23H32N4.HCl=400.99
4℃ ≧99%(HPLC) 50 mM in DMSO and to 50 mM in ethanol
516-94281 3767/10 CP 20961 10mg
- 3767/50 50mg
Non-immunogenic adjuvant; used to induce arthritis in Lewis (LEW) and DA rats.

cp-20961_3767.png

N,N-Dioctadecyl-N',N'-bis(2-hydroxyethyl)-1,3-diaminopropane
35607-20-6 C43H90N2O2=667.19
RT - 50 mM in ethanol with gentle warming
511-92891 3023/10 CP 31398 dihydrochloride 10mg
- 3023/50 50mg
p53 stabilizing agent. Stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53. Inhibits growth of small human tumor xenografts in vivo.

cp-31398-dihydrochloride_3023.png

N'-[2-[2-(4-Methoxyphenyl)ethenyl]-4-quinazolinyl]-N,N-dimethyl-1,3-propanediamine dihydrochloride
1217195-61-3 C22H26N4O2.2HCl=435.39
RT ≧99%(HPLC) 100 mM in water and to 100 mM in DMSO
- 6107/10 CP 424174 10mg
- 6107/50 50mg
Inhibitor of IL-1β post-translational processing (IC50 = 210 nM). Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.

cp-424174_6107.png

N-[[[4-Chloro-2,6-bis(1-methylethyl)phenyl]amino]carbonyl]-3-(1-hydroxy-1-methylethyl)benzenesulfonamide
210825-31-3 C22H29ClN2O4S=452.99
4℃ ≧98%(HPLC) 100 mM in ethanol and to 100 mM in DMSO
517-86021 3780/10 CP 471474 10mg
- 3780/50 50mg
Broad spectrum MMP inhibitor (IC50 values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice. cp-471474_3780.png
2-[[[4-(4-Fluorophenoxy)phenyl]sulfonyl]amino]-N-hydroxy-2-methylpropanamide
210755-45-6 C16H17FN2O5S=368.38
-20℃ ≧97%(HPLC) 100 mM in DMSO
551-21781 4556/10 CP 690550 citrate 10mg
- 4556/50 50mg
Potent JAK inhibitor (IC50 values are 1, 20, and 112 nM for JAK3, JAK2 and JAK1 respectively). Orally active immunosuppressant; exhibits efficacy in rodent rheumatoid arthritis models.

cp-690550-citrate_4556.png

(3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate
540737-29-9 C16H20N6O.C6H8O7=504.49
4℃ ≧99%(HPLC) 100 mM in DMSO
- 5973/10 CP 724714 10mg
- 5973/50 50mg
Potent and selective ErbB2 inhibitor (IC50 = 10 nM). Exhibits 500-1000-fold selectivity for ErbB2 over ErbB1 and other related RTKs. Induces G1 cell cycle arrest in an ErbB2-overexpressing human cancer cell line. Promotes tumor apoptosis. Induces tumor regression in a human tumor xenograft model. Displays no apparent toxic effect on cardiac tissue.

cp-724714_5973.png

2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
383432-38-0 C27H27N5O3=469.53
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
518-91681 4190/10 CP 775146 10mg
- 4190/50 50mg
Selective, high affinity PPARα agonist (Ki values are 24.5 nM for PPARα and >10 µM for PPARβ and PPARγ in vitro). Exhibits hypolipidemic activity in vivo.

cp-775146_4190

2-Methyl-2-[3-[(3S)-1-[2-[4-(1-methylethyl)phenyl]acetyl]-3-piperidinyl]phenoxy]-propanoic acid
702680-17-9 C26H33NO4=423.54
RT ≧99%(HPLC) 100 mM in DMSO
500-37861 1032/10 CP 93129 dihydrochloride 10mg
506-37863 1032/50 50mg
Potent and highly selective 5-HT1B agonist (Ki values are 8.1, 1100, 1500, 2900 and 7200 nM for 5-HT1B, 5-HT1D, 5-HT1A, 5-HT1c and 5-HT2, respectively). Reduces food intake and decreases body weight in rats.

cp-93129-dihydrochloride_1032

1,4-Dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrol[3,2-b]pyridin-5-one dihydrochloride
879089-64-2 C12H13N3O.2HCl=288.18
RT - 100 mM in water
519-91731 4236/10 CP 945598 hydrochloride 10mg
- 4236/50 50mg
Selective, high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively). Displays low affinity for CB2 receptors (Ki = 7600 nM).

cp-945598-hydrochloride_4236

1-[8-(2-Chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)piperidine-4-carboxamide hydrochloride
686347-12-6 C25H25Cl2N7O.HCl=546.88
4℃ ≧99%(HPLC) 20 mM in DMSO
514-85931 2893/10 CP 96345 10mg
- 2893/50 50mg
Potent and selective non-peptide NK1 receptor antagonist. Attenuates substance P-induced salivary response and inhibits neurogenic inflammation in vivo.

cp-96345_2893.png

(2S,3S)-N-(2-Methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-amine
132746-60-2 C28H32N2O=412.57
-20℃ ≧98%(HPLC) 20 mM in DMSO with gentle warming
511-91551 3417/10 CP 99994 dihydrochloride 10mg
- 3417/50 50mg
High affinity NK1 antagonist (Ki = 0.145 nM in vitro). Also displays high ex vivo binding potency in gerbil striatum (IC50 = 36.8 nM). Attenuates endothelium-dependent contraction induced by substance P.

cp-99994-dihydrochloride_3417.png

(2S,3S)-N-[(2-Methoxyphenyl)methyl]-2-phenyl-3-piperidinamine dihydrochloride
145148-39-6 C19H24N2O.2HCl=369.33
RT ≧99%(HPLC) 100 mM in water and to 50 mM in DMSO
- 5479/10 CRID3 sodium salt 10mg
- 5479/50 50mg
Potent NLRP3 inflammasome inhibitor; inhibits IL-1β (IC50 = 7.2 nM), IL-1α (IC50 = 12-18 nM) and IL-18 (IC50 = 10.3 nM) production. Selective for NLRP3 inflammasome over NLRC4 inflammasome and Toll-like receptor signaling. Inhibits inflammasome activation by soluble and crystalline NLRP3 stimuli. Reduces severity of experimental autoimmune encephalomyelitis, skin inflammation and airway inflammation in mice. Also glutathione S-transferase omega 1 inhibitor. Orally bioavailable. crid3-sodium-salt_5479.png
N-[[(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)amino]carbonyl]-4-(1-hydroxy-1-methylethyl)-2-furansulfonamide sodium salt
256373-96-3 C20H23N2NaO5S=426.46
4℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
- 4368/10 Crizotinib 10mg
- 4368/50 50mg
Potent inhibitor of c-MET and anaplastic lymphoma kinase (ALK) (cell IC50 values are 8.0 and 20 nM respectively). Selective for c-MET and ALK against >120 different kinases. Displays antitumor efficacy in multiple tumor models; inhibits c-MET-dependent proliferation, migration and invasion of human tumor cells in vitro. Orally bioavailable.

crizotinib_4368.png

3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
877399-52-5 C21H22Cl2FN5O=450.34
4℃ ≧99%(HPLC) 10 mM in DMSO and to 100 mM in 2eq.HCl
- 6025/10 (S)-Crizotinib 10mg
- 6025/50 50mg
Potent MTH1 inhibitor (IC50 = 72 nM). Induces DNA damage and disrupts nucleotide pool homeostasis in cancer cells. Also attenuates colony formation of KRAS-mutated PANC1 cells in vitro. Suppresses tumor growth 〜50% in a colon cancer carcinoma xenograft model.

s-crizotinib_6025.png

3-[(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
1374356-45-2 C21H22Cl2FN5O=450.34
RT ≧98%(HPLC) 50 mM in DMSO and to 20 mM in 1eq. HCl with gentle warming
- 3757/5 Dofetilide 5mg
- 3757/25 25mg
Selective potassium channel blocker. Blocks KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Displays class III antiarrhythmic properties.

dofetilide_3757.png

1-(4-Methanesulphonamidophenoxy)-2-[N-(4-methanesulphonamidophenethyl)-N-methylamino]ethane
115256-11-6 C19H27N3O5S2=441.56
RT ≧99%(HPLC) 100 mM in DMSO
588-77621 0518/10 EBPC 10mg
- 0518/50 50mg
Potent aldose reductase inhibitor. Improves the cytotoxicity of anticancer reagents such as cisplatin (Cat.No. 2251) and doxorubicin (Cat.No. 2252) in HeLa cervical carcinoma cells through an increase in ERK activity. ebpc_0518.png
Ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate
4450-98-0 C14H15NO4=261.28
4℃ ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
- 3862/5 Eletriptan hydrobromide 5mg
- 3862/25 25mg
Orally active, selective 5-HT1B/1D receptor agonist. Produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity.

eletriptan-hydrobromide_3862.png

3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole hydrobromide
177834-92-3 C22H26N2O2S.HBr=463.43
RT ≧99%(HPLC) 100 mM in DMSO
510-91761 4276/10 ERB 041 10mg
- 4276/50 50mg
Potent Erβ agonist; displays >200-fold selectivity for Erβ over Erα (IC50 values are 5 and 1216 nM for human ERβ and ERα; 3.1 and 620 nM for rat ERβ and ERα; and 3.7 and 750 nM for mouse Erβ and Erα respectively). erb-041_4276.png
7-Ethenyl-2-(3-fluoro-4-hydroxyphenyl)-5-benzoxazolol
524684-52-4 C15H10FNO3=271.24
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
515-94251 3759/10 Exemestane 10mg
- 3759/50 50mg
Irreversible steroidal aromatase inhibitor (IC50 = 20 nM). Destabilizes aromatase and lowers estrogen levels; orally active.

exemestane_3759.png

6-Methyleneandrosta-1,4-diene-3,17-dione
107868-30-4 C20H24O2=296.4
-20℃ ≧99%(HPLC) 100 mM in DMSO and to 75 mM in ethanol
519-94271 3764/50 Fluconazole 50mg
Triazole antifungal agent. Effective against Candida strains in vitro and in vivo.

fluconazole_3764.png

2-(2,4-Difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol
86386-73-4 C13H12F2N6O=306.27
4℃ - 100 mM in DMSO and to 100 mM in ethanol
- 0806/10 Gabapentin 10mg
578-69631 0806/50 50mg
Anticonvulsant with several possible mechanisms of action. Increases GABA in the brain and binds to a novel site associated with voltage-sensitive Ca2+ channels. Prevents neuronal death and is antinociceptive and anxiolytic. gabapentin_0806.png
1-(Aminomethyl)cyclohexaneacetic acid
60142-96-3 C9H17NO2=171.24
4℃ ≧99%(HPLC) 100 mM in water with gentle warming
512-91601 4165/10 Gisadenafil besylate 10mg
- 4165/50 50mg
Potent PDE5 inhibitor (IC50 = 1.23 nM). Shows >100-fold selectivity for PDE5 over PDE6. Orally bioavailable.

gisadenafil-besylate_4165.png

5-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]-3-pyridinyl]-3-ethyl-2,6-dihydro-2-(2-methoxyethyl)-7H-pyrazolo[4,3-d]pyrimidin-7-one benzenesulfonate
334827-98-4 C23H33N7O5S.C6H6O3S=677.79
RT ≧99%(HPLC) 10 mM in water and to 100 mM in DMSO
511-96431 2332/10 (+)-Igmesine hydrochloride 10mg
- 2332/50 50mg
Selective σ1 receptor ligand (KD = 19.1 nM), with little or no activity at σ2 receptors (IC50 > 1000 nM). Inhibits the NMDA-induced increase in cGMP in a concentration-dependent manner (IC50 value is approximately 100 nM). Weak inhibitor of brain 5-HT uptake in vitro. Exhibits neuroprotective and antidepressant effects. plus-igmesine-hydrochloride_2332.png
(R)-(+)-N-Cyclopropylmethyl-α-ethyl-N-methyl-α-[(2E)-3-phenyl-2-propenyl)benzenemethanamine hydrochloride
130152-35-1 C23H29N.HCl=355.94
-20℃ ≧98%(HPLC) 50 mM in DMSO
- 5806/10 ISOX DUAL 10mg
- 5806/50 50mg
Dual CBP/p300 and BRD4 bromodomain inhibitor (IC50 values are 0.65 and 1.5 µM for CBP and BRD4 respectively). Downregulates IL-6, IL-1β and IFN-β in macrophages.

isox-dual_5806.png

[3-[4-[2-[5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-1H-1,3-benzodiazol-2-yl]ethyl]phenoxy]propyl]dimethylamine
- C31H41N5O3=531.69
4℃ ≧98%(HPLC) 100 mM in 1eq. HCl and to 50 mM in DMSO
- 5808/10 ISOX INACT 10mg
- 5808/50 50mg
Negative control for PF CBP1 (Cat. No. 5801). Exhibits negligible activity at CBP and BRD4.

isox-inact_5808.png

5-(Dimethyl-1,2-oxazol-4-yl)-2-[2-(4-methoxyphenyl)ethyl]--4,6-dimethyl-1-[2-(morpholin-4-yl)ethyl]-1H-1,3-benzodiazole
- C29H36N4O3=488.62
4℃ ≧98%(HPLC) 50 mM in DMSO and to 20 mM in ethanol
516-85991 3765/10 Linezolid 10mg
Oxazolidinone antibiotic. Inhibits bacterial protein synthesis prior to chain initiation. Displays potent antibacterial activity against a variety of multidrug-resistant gram-positive microbes in vitro and in vivo.

linezolid_3765.png

N-[[(5S)-3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide
165800-03-3 C16H20FN3O4=337.35
RT ≧99%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
518-91561 3763/1 MCOPPB trihydrochloride 1mg
- 3763/10 10mg
High affinity NOP receptor agonist (pKi = 10.07 for the human NOP receptor). Exhibits anxiolytic effects with no effect on memory or locomotion. Regarded as one of the most potent, non-peptide NOP full agonists in vitro.

mcoppb-trihydrochloride_3763.png

1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-(3R)-3-piperidinyl-1H-benzimidazole trihydrochloride
1108147-88-1 C26H40N4.3HCl=534.05
-20℃ ≧99%(HPLC) 30 mM in water and to 60 mM in DMSO
558-21791 4819/50 Methylprednisolone 50mg
Glucocorticoid receptor (GR) agonist. Displays anti-inflammatory and antioxidant properties. Attenuates apoptosis in oligodendrocytes after injury stimuli. Upregulates expression of Bcl-XL via direct binding of the GR/STAT5 complex. Neuroprotective.

methylprednisolone_4819.png

11β,17β,21-Trihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione
83-43-2 C22H30O5=374.47
4℃ ≧99%(HPLC) 100 mM in DMSO
513-86001 3766/10 Nelfinavir mesylate 10mg
- 3766/50 50mg
Orally active human immunodeficiency virus protease inhibitor. Potently inhibits HIV-1 protease (Ki = 2 nM) in vitro.

nelfinavir-mesylate_3766.png

(3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2- hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide methanesulfonate
159989-65-8 C32H45N3O4S.CH4O3S=663.89
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
517-94191 2599/10 OSU 6162 hydrochloride 10mg
- 2599/50 50mg
Dopamine stabilizer; lacks high affinity for various neuroreceptors in vitro (Ki values are 447 and 1305 nM for D2 and D3 receptors respectively and > 1 µM for other targets). Exhibits high D2 receptor occupancy in vivo; highly active on dopamine synthesis and turnover. Induces stabilizing effects on psychomotor function in behavioral tests without inducing hypolocomotion or catalepsy.

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(3S)-3-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride
156907-84-5 C15H23NO2S.HCl=317.87
4℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
518-91701 4192/10 PD 0325901 10mg
- 4192/50 50mg
Potent MEK1 and MEK2 inhibitor. Inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). Inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. Also inhibits production of proangiogenic cytokines such as VEGF. Enhances generation of induced pluripotent stem cells (iPSCs). Orally active.

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N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
391210-10-9 C16H14F3IN2O4=482.19
-20℃ ≧99%(HPLC) 25 mM in DMSO
- 4786/10 PD 0332991 isethionate 10mg
- 4786/50 50mg
Potent Cdk4/6 inhibitor (IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 µM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.

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6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one isethionate salt
827022-33-3 C24H29N7O2.C2H6O4S=573.66
RT ≧98%(HPLC) 100 mM in water and to 10 mM in DMSO
510-94201 2606/10 PD 144418 oxalate 10mg
- 2606/50 50mg
High affinity, selective σ1 ligand (Ki values are 0.08 and 1377 nM for σ1 and σ2 respectively). Displays no significant activity at a wide range of other receptors, ion channels and enzymes. Antagonizes mescaline-induced scratching in mice following i.p. administration. Also attenuates cocaine-induced hyperactivity in mice.

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1,2,3,6-Tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine oxalate
154130-99-1 C18H22N2O.C2H2O4=372.42
RT ≧98%(HPLC) 50 mM in DMSO
518-85951 3724/10 PD 161570 10mg
- 3724/50 50mg
Selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). Inhibits FGFR receptor phosphorylation (IC50 = 622 nM) and growth of A121 cells in vitro.

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N-[6-(2,6-Dichlorophenyl)-2-[[4-(diethylamino)butyl]amino]pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
192705-80-9 C26H35Cl2N7O=532.51
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
516-94301 3785/1 PD 166285 dihydrochloride 1mg
- 3785/10 10mg
Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFRβ) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G2 checkpoint.

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6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one dihydrochloride
212391-63-4 C26H27Cl2N5O2.2HCl=585.35
RT ≧99%(HPLC) 100 mM in DMSO
511-94231 3044/10 PD 173074 10mg
- 3044/50 50mg
Selective FGFR1 and FGFR3 inhibitor (IC50 values are 5, 21.5, 〜100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively, and > 50000 nM for EGFR, InsR, MEK and PKC). Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis. Inhibits proliferation and differentiation of oligodendrocyte progenitors. Suppresses cell proliferation in cell lines expressing mutated FGFR3 protein. Blocks tumor growth in H510 and H69 SCLC xenograft models.

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N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea
219580-11-7 C28H41N7O3=523.67
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
555-21821 4965/10 PD 180970 10mg
ATP-competitive inhibitor of p210bcr/abl tyrosine kinase; selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. Inhibits in vivo tyrosine phosphorylation of Gab2, CrkL and p210bcr/abl (IC50 values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/abl autophosphorylation in vitro (IC50 = 5 nM). Also potently inhibits c-Src and KIT (IC50 values are 0.8 and 50 nM, respectively).

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6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
287204-45-9 C21H15Cl2FN4O=429.27
4℃ ≧98%(HPLC) 50 mM in DMSO
512-90143 4237/10 PD 184352 10mg
516-90141 4237/50 50mg
Selective MEK inhibitor (Ki = 300 nM in vitro). Suppresses FGF-mediated angiogenesis in vivo and decreases VEGF expression. Enhances the therapeutic efficacy of taxol (Cat. No. 1097) in vivo. Orally active.

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2-[(2-Chloro-4-iodophenyl)amino]-N-cyclopropylmethoxy)-3,4-difluorobenzamide
212631-79-3 C17H14ClF2IN2O2=478.66
4℃ - 100 mM in DMSO and to 25 mM in ethanol
517-94211 2694/1 PD 407824 1mg
- 2694/10 10mg
Selective inhibitor of checkpoint kinases Chk1 and Wee1 (IC50 values are 47 and 97 nM respectively). Displays selectivity over a range of other protein kinases; IC50 values are 3.4, 3.75, > 5, > 50, > 50 and > 50 µM for PKC, CDK4, other CDKs, c-Src, PDGFR and FGFR respectively.

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9-Hydroxy-4-phenyl-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione
622864-54-4 C20H12N2O3=328.32
4℃ ≧98%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
559-02781 4821/10 PF 03814735 10mg
- 4821/50 50mg
ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5 nM for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are approximately 20, 50 and 150 nM respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Orally available.

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N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
942487-16-3 C23H25F3N6O2=474.48
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
513-91751 4239/10 PF 04217903 mesylate 10mg
- 4239/50 50mg
Highly selective, high affinity MET inhibitor (Ki = 6-7 nM against wild type c-Met). Displays >1000-fold selectivity for c-Met over a panel of 208 kinases.

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4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol mesylate
956906-93-7 C19H16N8O.CH3SO3H=468.49
4℃ ≧98%(HPLC) 100 mM in DMSO
552-02771 4818/10 PF 04418948 10mg
- 4818/50 50mg
Potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 µM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

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1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
1078166-57-0 C23H20FNO5=409.41
-20℃ ≧99%(HPLC) 100 mM in DMSO
- 5915/10 PF 04449613 10mg
Potent PDE9 inhibitor (IC50 = 22 nM). Also exhibits a high affinity for cGMP (Km 〜170 nM). Brain penetrant.

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1,5-Dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
1236858-52-8 C21H25N5O3=395.45
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 10 mM in 1eq. HCl with gentle warming
556-02791 4916/10 PF 04885614 10mg
- 4916/50 50mg
Potent NaV1.8 inhibitor (IC50 = 53 nM for human NaV1.8 channel). Exhibits selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNaV1.2 and hNaV1.5 (IC50 values are 4.2, 7.0, 11, 16 and 27 µM respectively). Orally bioavailable.

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1-Methyl-[1-[4-(4-trifluoromethoxy)phenyl]-imidazol-2-yl]-ethanamine
- C13H14F3N3O=285.26
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 4820/5 PF 04691502 5mg
- 4820/25 25mg
Potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (Ki values are 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, γ, β, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration greater than or equal to 10 µM) including hVps34, PI 3-K downstream kinases, and MAPK family members. Orally available. Induces robust cell cycle arrest at the G1 phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models.

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2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
1013101-36-4 C22H27N5O4=425.48
-20℃ ≧98%(HPLC) 100 mM in DMSO
- 5931/10 PF 05089771 10mg
- 5931/50 50mg
Potent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 µM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.

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4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
1430806-04-4 C18H12Cl2FN5O3S2.C7H8O3S=672.56
RT ≧98%(HPLC) 100 mM in DMSO
- 6003/10 PF 05105679 10mg
Selective TRPM8 blocker (IC50 = 103 nM). Exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. Reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. Orally bioavailable.

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3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
1398583-31-7 C26H21FN2O3=428.45
RT ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5790/10 PF 05175157 10mg
- 5790/50 50mg
Acetyl-CoA carboxylase (ACC) 2 and 1 inhibitor (IC50 values are 45 and 98 nM, respectively). Reduces hepatic and skeletal muscle malonyl-CoA levels in rats. Also inhibits hepatic de novo lipogenesis and reduces whole body respiratory exchange ratio in rats. Orally bioavailable.

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1,4-Dihydro-1'-[2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4'-piperidin]-7(6H)-one
1301214-47-0 C23H27N5O2=405.49
4℃ ≧98%(HPLC) 50 mM in DMSO and to 20 mM in ethanol
550-02331 4823/10 PF 05212384 10mg
Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10 µM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.

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N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]urea
1197160-78-3 C32H41N9O4=615.73
-20℃ ≧98%(HPLC) 5 mM in DMSO with gentle warming
- 5752/10 PF 06260933 dihydrochloride 10mg
- 5752/50 50mg
MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.

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5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride
- C16H13ClN4.2HCl=369.68
RT ≧98%(HPLC) 100 mM in water and to 20 mM in DMSO
- 6115/10 PF 06273340 10mg
Potent and selective pan-Trk inhibitor (IC50 values are 1, 2 and 6 nM for Trk C, B and A, respectively). Selective for Trk over a panel of ion channels, receptors and other enzymes. Peripherally restricted. Exhibits efficacy in a rodent model of inflammatory pain. Orally bioavailable.

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N-[5-[[2-Amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-2-pyridineacetamide
1402438-74-7 C23H22ClN7O3=479.93
RT ≧98%(HPLC) 100 mM in DMSO
- 6004/10 PF 06281355 10mg
- 6004/50 50mg
Selective myeloperoxidase (MPO) inhibitor (IC50 = 1.5 µM in LPS-stimulated human whole blood). Selective for MPO over a panel of 50 receptors, enzymes, ion channels and transporters, including thyroid peroxidase. Inhibits MPO activity in peritoneal lavage and plasma in a murine peritonitis model. Also reduces lung edema in a murine pulmonary immune complex vasculitis model. Orally bioavailable.

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6-(2,5-Dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide
1435467-38-1 C14H15N3O4S=321.35
RT ≧98%(HPLC) 20 mM in DMSO with gentle warming
- 5716/10 PF 06447475 10mg
- 5716/50 50mg
Potent LRRK2 inhibitor (IC50 = 3 nM). Attenuates α-synuclein-induced dopaminergic neurodegeneration and neuroinflammation in G2019S-LRRK2 expressing rats. Also neuroprotective in wild type rats. Brain penetrant.

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3-[4-(4-Morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
1527473-33-1 C17H15N5O=305.33
4℃ ≧98%(HPLC) 50 mM in DMSO
- 6114/10 PF 06409577 10mg
- 6114/50 50mg
Potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively). Exhibits minimal off target effects on a panel of receptors, ion channels, PDEs and kinases. Demonstrates efficacy in a preclinical model of diabetic nephropathy. Orally bioavailable.

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6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid
1467057-23-3 C19H16ClNO3=341.79
RT ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
- 5640/10 PF 06463922 10mg
- 5640/50 50mg
High affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.

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(10R)-7-Amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile
1454846-35-5 C21H19FN6O2=406.41
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
558-02751 4710/10 PF 06465469 10mg
- 4710/50 50mg
Potent inhibitor of interleukin-2 inducible T cell kinase (ITK) (IC50 = 2 nM). Also exhibits inhibitory activity against Bruton's tyrosine kinase (BTK) (IC50 = 2 nM). Displays nanomolar potencies in a cell-based IP1 assay and human whole blood assay (IC50 values are 31 and 48 nM respectively).

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(R)-3-(1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(3-methyl-4-(1-methylethyl))benzamide
1407966-77-1 C30H33N7O2=523.634
4℃ ≧95%(HPLC) 5 mM in DMSO with gentle warming
- 6169/10 PF 06726304 acetate 10mg
Highly potent and SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50 = 0.7 nM). Inhibits proliferation of Karpas-422 cells (non-Hodgkin's lymphoma) in vitro, and halts tumor growth and reduces intratumoral H3K27Me3 levels in mice.

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5,8-Dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone acetate
- C22H21Cl2N3O3.C2H4O2=506.38
RT ≧97%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
516-91741 4238/10 PF 184 10mg
Potent and selective IKKβ inhibitor (IC50 = 37 nM). Displays selectivity over 85 other kinases. Inhibits IL-1β-induced TNF-α production in a steroid-insensitive in vitro model of oxidative stress.

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8-[[[5-Chloro-2-[3,4-dimethyl-3,4-bis(hydroxymethyl)-1-pyrrolidinyl]-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide
1187460-81-6 C32H32ClFN6O4=619.09
4℃ ≧98%(HPLC) 100 mM in DMSO
- 5751/10 PF 3084014 hydrobromide 10mg
- 5751/50 50mg
Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs.

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(2S)-2-[[(2S)-6,8-Difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-N-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1H-imidazol-4-yl]pentanamide dihydrobromide
1962925-29-6 C27H41F2N5O.HBr=651.47
RT ≧98%(HPLC) 10 mM in water with gentle warming and to 100 mM in DMSO
517-95931 4279/10 PF 3644022 10mg
Potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.

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(10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
1276121-88-0 C21H18N4OS=374.46
4℃ ≧98%(HPLC) 40 mM in DMSO
515-91691 4191/10 PF 3716556 10mg
- 4191/50 50mg
H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays); more potent in acidic conditions. Highly selective for H+,K+-ATPase in vitro; displays no activity at Na+,K+-ATPase. Also displays selectivity for H+,K+-ATPase over a range of 50 receptors and ion channels (IC50 > 10 µM). Inhibits gastric acid secretion in rat and dog models.

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8-[[(4R)-3,4-Dihydro-5-methyl-2H-1-benzopyran-4-yl]amino]-N-(2-hydroxyethyl)-N,2-dimethyl-imidazo[1,2-a]pyridine-6-carboxamide
928774-43-0 C22H26N4O3=394.47
-20℃ ≧98%(HPLC) 100 mM in DMSO
- 6005/10 PF 3758309 dihydrochloride 10mg
- 6005/50 50mg
Potent PAK4 inhibitor (IC50 = 1.3 nM; Kd = 2.7 nM). Inhibits proliferation and anchorage-independent growth of a panel of tumor cell lines in vitro. Suppresses growth of human HCT116 and A549 tumor cell xenografts in mice. Orally available.

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N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide dihydrochloride
- C25H30N8OS.2HCl=563.55
-20℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
519-91611 4175/10 PF 3845 10mg
- 4175/50 50mg
Selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 µM). Reduces inflammatory pain via a cannabinoid receptor-dependent mechanism. Highly efficacious and selective in vivo. Displays no activity at FAAH-2 (IC50 >10 µM).

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N-3-Pyridinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]-1-piperidinecarboxamide
1196109-52-0 C24H23F3N4O2=456.46
4℃ ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
510-95921 3354/10 PF 429242 10mg
- 3354/50 50mg
Reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 µM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 µM). Also displays antiviral activity. Cell permeable.

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4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide
947303-87-9 C25H35N3O2.2HCl=482.49
RT ≧97%(HPLC) 50 mM in water and to 50 mM in DMSO
511-94351 4278/10 PF 431396 10mg
Dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively). Promotes osteoblast recruitment and activity, and stimulates bone formation in ovariectomized rats.

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N-Methyl-N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
717906-29-1 C22H21F3N6O3S=506.5
4℃ ≧98%(HPLC) 50 mM in DMSO
- 4032/5 PF 4708671 5mg
- 4032/25 25mg
Cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) (Ki = 20 nM; IC50 = 160 nM). Suppresses the S6K1-mediated phosphorylation of S6, Rictor and mTOR in response to IGF1; displays no effect on the activity of RSK and MSK in vivo. Exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro.

pf-4708671_4032

2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole
1255517-76-0 C19H21F3N6=390.41
4℃ ≧98%(HPLC) 50 mM in DMSO and to 50 mM in ethanol
515-92171 4277/10 PF 477736 10mg
- 4277/50 50mg
Selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Enhances docetaxel (Cat. No. 4056) efficacy in tumor cells and xenografts.

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(R)-α-Amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide
952021-60-2 C22H25N7O2=419.48
4℃ ≧99%(HPLC) 75 mM in DMSO
558-21811 4900/10 PF 4778574 10mg
Positive allosteric modulator of AMPA receptors (Ki = 85 nM). Prevents ketamine-induced working memory impairments. Brain penetrant.

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N-[(3R,4S)-3-[4-(5-cyano-2-thienyl)phenyl]tetrahydro-2H-pyran-4-yl]-2-propanesulfonamide
1219633-99-4 C19H22N2O3S2=390.52
4℃ ≧98%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
518-94361 4281/10 PF 4800567 hydrochloride 10mg
- 4281/50 50mg
Selective casein kinase 1ε inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock.

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3-[(3-Chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine hydrochloride
1391052-28-0 C17H18ClN5O2.HCl=396.27
RT ≧99%(HPLC) 100 mM in DMSO
516-97721 4252/10 PF 4981517 10mg
- 4252/50 50mg
Potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 µM for CYP3A4, CYP3A5 and CYP3A7 respectively).

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(1-Methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine)
1390637-82-7 C26H32N8=456.59
4℃ ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
513-97731 4362/10 PF 5081090 10mg
Potent antibacterial agent which disrupts lipid bilayer synthesis through inhibition of LpxC (IC50 = 1.1 nM in Pseudomonas aeruginosa); effective against a range of gram negative bacteria.

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R)-4-(2-Fluoro-4-methoxyphenyl)-N-hydroxy-α-methyl-α-(methylsulfonyl)-2-oxo-1(2H)-pyridinebutanamide
1312473-63-4 C18H21FN2O6S=412.43
-20℃ ≧98%(HPLC) 100 mM in DMSO
- 5262/10 PF 5274857 hydrochloride 10mg
- 5262/50 50mg
High affinity and selective Smoothened (Smo) receptor antagonist (Ki = 4.6 nM). Exhibits >1000-fold selectivity for Smo over a panel of other receptors, ion channels and enzymes. Inhibits Shh-induced Hedgehog signaling in MEF cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.

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1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
1613439-62-5 C20H25ClN4O3S.HCl=473.42
RT ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
- 5754/10 PF 543 hydrochloride 10mg
- 5754/50 50mg
Potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice.

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(2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
1706522-79-3 C27H31NO4S.HCl=502.07
RT ≧98%(HPLC) 10 mM in water with gentle warming and to 100 mM in DMSO
517-80661 3239/10 PF 573228 10mg
- 3239/50 50mg
Potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM). Displays 50 - 250-fold selectivity for FAK over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro.

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3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
869288-64-2 C22H20F3N5O3S=491.49
4℃ ≧98%(HPLC) 100 mM in DMSO
- 5939/10 PF 6274484 10mg
- 5939/50 50mg
High affinity and potent covalent EGFR kinase inhibitor (Ki = 0.14 nM). Inhibits autophosphorylation of WT and mutant EGFR in tumor cells (IC50 values are 5.8 and 6.6 nM, respectively).

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N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-2-propenamide
1035638-91-5 C18H14ClFN4O2=372.78
-20℃ ≧98%(HPLC) 100 mM in DMSO
- 5917/10 PF 9184 10mg
- 5917/50 50mg
Potent microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor (IC50 values are 16.5 and 1080 nM for human and rat mPGES-1, respectively). Exhibits >6500-fold selectivity for mPGES-1 over COX-1 and COX-2. Inhibits IL-1β-induced PGE2 synthesis in vitro.

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N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
1221971-47-6 C21H14Cl2N2O4S=461.32
-20℃ ≧98%(HPLC) 100 mM in DMSO
557-21761 4419/10 PF 945863 10mg
Macrolide antibiotic. Active against multidrug resistant respiratory tract bacterial strains. Does not have the hepatotoxic side effects associated with telithromycin. Orally active.

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(3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-4-Ethyloctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-[1-[(1R)-1-(1,8-naphthyridin-4-yl)ethyl]-3-azetidinyl]-10-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-2H-oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)tetrone
893556-85-9 C44H65N5O10=824.01
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
517-94331 3923/10 PF 998425 10mg
Selective non-steroidal androgen receptor (AR) antagonist (IC50 values are 26 nM and 90 nM in AR binding assays and cellular assays respectively). Displays low affinity for progesterone receptor (IC50 > 10 µM). Active in vivo.

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4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile
1076225-27-8 C14H14F3NO=269.26
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5801/10 PF CBP1 10mg
- 5801/50 50mg
Selective CBP/p300 bromodomain inhibitor (IC50 values are 125 and 363 nM, respectively). Exhibits >100-fold selectivity for CBP over BRD4. Also exhibits selectivity over a panel of other bromodomains. Reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. Also downregulates RGS4 expression in primary cortical neurons in vitro.

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5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole
- C29H36N4O3=488.62
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5866/10 PH 797804 10mg
- 5866/50 50mg
Potent and selective p38α/β inhibitor (IC50 values are 26 and 102 nM, respectively). Exhibits >100-fold selectivity for p38α/β over 71 other kinases, enzymes and GPCRs, including p38γ, p38δ, JNK and ERK2. Inhibits LPS-induced TNFα production in U937 monocytes in vitro. Suppresses acute and chronic inflammatory responses in rat models of arthritis. Orally active.

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(-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide
1358027-80-1 C22H19BrF2N2O3=477.3
-20℃ ≧98%(HPLC) 50 mM in DMSO
517-88081 3092/10 PHA 543613 hydrochloride 10mg
Potent α7 nAChR agonist that displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.

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N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide hydrochloride
478149-53-0 C15H17N3O2.HCl=307.78
4℃ ≧98%(HPLC) 100 mM in water and to 25 mM in DMSO
511-52091 2693/10 PHA 665752 10mg
- 2693/50 50mg
Potent, selective and ATP-competitive inhibitor of MET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

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(2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine
477575-56-7 C32H34Cl2N4O4S=641.61
4℃ ≧98%(HPLC) 100 mM in DMSO
510-943211 3919/10 SC 236 10mg
- 3919/50 50mg
Selective COX-2 inhibitor (IC50 values are 0.005 and 17.8 µM for COX-2 and COX-1 respectively). Displays anti-inflammatory properties and potent antimetastatic activity against both experimental metastases and spontaneous metastases arising following primary tumor excision.

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4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide
170569-86-5 C16H11ClF3N3O2S=401.79
RT ≧99%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
519-85981 3758/10 SC 51089 10mg
- 3758/50 50mg
Selective EP1 prostanoid receptor antagonist (Ki values are 1.3, 11.2, 17.5, 61.1, > 100, > 100, > 100, >100 and > 100 µM for EP1, TP, EP3, EP2, EP4, FP and DP receptors respectively). Attenuates PGE2-induced neuronal cell death in vitro and slows tumor growth in vivo.

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8-Chlorodibenz(Z)[b,f][1,4]oxazepine-10(11H)-carboxylic acid 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide hydrochloride
146033-02-5 C22H19ClN4O3.HCl=459.33
-20℃ ≧99%(HPLC) 100 mM in DMSO
511-91671 4189/10 SC 26196 10mg
- 4189/50 50mg
Selective Δ6 desaturase inhibitor (IC50 = 0.2 µM in vitro). Displays selectivity over Δ5 and Δ9 desaturases (IC50 values are >200 µM in vitro). Exhibits anti-inflammatory properties in a mouse edema model. Eliminates CSCs from ovarian cancer cell lines and inhibits sphere formation in vitro.

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α,α-Diphenyl-4-[(3-pyridinylmethylene)amino]-1-piperazinepentanenitrile
218136-59-5 C27H29N5=423.55
-20℃ ≧98%(HPLC) 25 mM in DMSO
514-94221 2791/10 SC 51322 10mg
- 2791/50 50mg
Potent EP1 prostanoid receptor antagonist (Ki = 13.8 nM). Displays analgesic properties in vivo.

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8-Chloro-2-[3-[(2-furanylmethyl)thio]-1-oxopropyl]-dibenz(Z)[b,f][1,4]oxazepine-10(11H)-carboxylic acid hydrazide
146032-79-3 C22H20ClN3O4S=457.93
4℃ ≧98%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
518-94241 3107/10 SC 57461A 10mg
- 3107/50 50mg
Potent and selective inhibitor of LTA4 hydrolase. Does not inhibit other enzymes of the arachidonic acid cascade including COX-1, COX-2, LTC4 synthase and 5-lipoxygenase. Potently inhibits LTB4 production in whole blood (IC50 = 49 nM). Orally active.

sc-57461a_3107

N-methyl-N-[3-[4-(phenylmethyl)phenoxy]propyl]-β-alanine hydrochloride
423169-68-0 C20H25NO3.HCl=363.88
4℃ ≧98%(HPLC) 25 mM in water and to 100 mM in DMSO
511-85941 2895/10 SC 58125 10mg
- 2895/50 50mg
Selective cyclooxygenase 2 (COX-2) inhibitor (IC50 values are 0.04 and >100 µM for COX-2 and COX-1 respectively). Anti-inflammatory; blocks edema and hyperalgesia in vivo following an inflammatory insult, without causing gastric mucosal damage. Also displays antitumor activity.

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5-(4-Fluorophenyl)-1-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole
162054-19-5 C17H12F4N2O2S=384.35
4℃ ≧98%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
- 4775/10 SD 2590 hydrochloride 10mg
- 4775/50 50mg
Potent MMP inhibitor (IC50 values are <0.1, <0.1, 0.18, 1.7, 13 and 28.7 nM for MMP-2, -13, -9, -8, -14 and -3 respectively). Exhibits 100,000-fold selectivity for MMP-2 and -13 over MMP-1. Reduces left ventricular dilation in a myocardial infarction rat model. Orally bioavailable.

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N-Hydroxy-1-(2-methoxyethyl)-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonyl]-4-piperidinecarboxamide hydrochloride
226395-93-3 C22H25F3N2O7S.HCl=554.96
-20℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
518-31621 2395/10 Sertraline hydrochloride 10mg
- 2395/50 50mg
Potent, orally active selective serotonin re-uptake inhibitor (SSRI); antidepressant.

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(1S,4S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride
79559-97-0 C17H17Cl2N.HCl=342.69
RT ≧99%(HPLC) 5 mM in water and to 100 mM in DMSO
- 3784/5 Sildenafil citrate 5mg
- 3784/25 25mg
Orally active, potent inhibitor of phosphodiesterase 5 (PDE5) (IC50 = 4 nM). Enhances nitric oxide-dependent relaxation of human corpus cavernosum in vitro.

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1-[[3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate
171599-83-0 C22H30N6O4S.C6H8O7=666.7
RT ≧99%(HPLC) 100 mM in DMSO
513-91631 4185/10 Sonepiprazole 10mg
- 4185/50 50mg
Selective, high affinity antagonist for the rat and human dopamine D4 receptor (Ki = 10 nM). Exhibits low affinity at other monoamine receptors (Ki > 2000 nM). Induces c-fos gene expression in medial prefrontal cortex in a similar manner to clozapine (Cat. No. 0444). Brain penetrant and orally available.

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4-[4-[2-[(1S)-3,4-Dihydro-1H-2-benzopyran-1-yl)ethyl]-1-piperazinyl]-benzenesulfonamide
170858-33-0 C21H27N3O3S=401.52
4℃ ≧98%(HPLC) 100 mM in DMSO
514-91541 2773/10 Sumanirole maleate 10mg
- 2773/50 50mg
High affinity D2 receptor agonist (EC50 values are between 17 and 75 nM in cell-based assays). Displays >200-fold selectivity for the D2 receptor against other dopamine receptor subtypes (Ki values are 9.0, 1940, >2190 and >7140 for D2, D3, D4 and D1 receptors respectively). More recently reported to be around 32-fold selective for D2 over D3 receptors (Ki values are 17.1 and 546 nM respectively). Exhibits antiParkinsonian activity.

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(R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (2Z)-2-butenedioate
179386-44-8 C11H13N3O.C4H4O4=319.31
-20℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
510-86011 3768/10 Sunitinib malate 10mg
- 3768/50 50mg
Potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.

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N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-2-hydroxybutanedioate salt
341031-54-7 C22H27FN4O2.C4H6O5=532.56
4℃ ≧99%(HPLC) 25 mM in DMSO
- 5264/10 Temsirolimus 10mg
mTOR inhibitor; inhibits tumor growth in breast cancer cell lines (IC50 values are 1.6 and 4.3 nM for SKBr3 and BT474, respectively). Inhibits HIF-1α-mediated VEGF production in breast cancer cell lines (BT474 and MDA-MB-231). Directly inhibits serum and VEGF mediated endothelial cell proliferation and morphogenesis in vitro and vessel formation in vivo. Causes G1/S cell cycle arrest in multiple cancer cell lines. Antiangiogenic. Activates autophagy.

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Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]
162635-04-3 C56H87NO16=1030.29
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5960/10 TMI 1 10mg
- 5960/50 50mg
Adam 17 (TACE) and MMP inhibitor (IC50 values are 3, 4.7, 6.6, 8.4, 12, 26 and 26 nM for MMP-13, MMP-2, MMP-1, ADAM 17, MMP-9, MMP-7 and MMP-14, respectively). Suppresses TNF-α production in an acute LPS-mouse model. Reduces severity score in an in vivo model of rheumatoid arthritis. Displays selective cytotoxicity to tumor cells and cancer stem cells in vitro. Induces tumor apoptosis in a breast cancer in vivo model. Orally bioavailable.

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(3S)-4-[[4-(2-Butyn-1-yloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-3-thiomorpholinecarboxamide
287403-39-8 C17H22N2O5S2=398.49
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
- 3909/10 Toceranib 10mg
- 3909/50 50mg
Potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki = 0.5 µM). Effective in vivo.

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5-[(Z)-(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(1-pyrrolidinyl)ethyl]-1H-pyrrole-3-carboxamide
356068-94-5 C22H25FN4O2=396.46
-20℃ ≧98%(HPLC) 10 mM in DMSO with gentle warming
512-94261 3761/10 Tolterodine L-tartrate 10mg
- 3761/50 50mg
High affinity muscarinic receptor antagonist (Ki = 3.3 nM). Active at all muscarinic receptor subtypes (M1 - M5); exhibits a greater effect on the bladder than salivary glands in vivo.

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2-[(1R)-3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-methylphenol (2R,3R)-2,3-dihydroxybutanedioate
124937-52-6 C22H31NO.C4H6O6=475.57
4℃ ≧99%(HPLC) 10 mM in water and to 100 mM in DMSO
516-91621 4184/10 Torcetrapib 10mg
- 4184/50 50mg
Inhibitor of cholesteryl ester transfer protein (CETP). Also impairs endothelial function in vivo; induces hypertension and inhibits acetylcholine-induced vasodilation in rabbit central ear artery.

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(2R,4S)-4-[[[3,5-bis(Trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinoline-1-carboxylic acid ethyl ester
262352-17-0 C26H25F9N2O4=600.47
RT ≧99%(HPLC) 50 mM in DMSO
511-86041 3863/10 Trovafloxacin mesylate 10mg
- 3863/50 50mg
Fluoroquinolone antibiotic. Inhibits bacterial DNA topoisomerase IV and DNA gyrase and forms a stable quinolone-DNA complex with these enzymes which reversibly inhibits DNA synthesis. Displays potent activity against gram-positive and gram-negative bacteria. Increases the production of mitochondrial NO in immortalized hepatocytes; also increases mitochondrial Ca2+. Inhibits Panx-1 (IC50 〜 4µM).

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7-[(1α,5α,6α)-6-Amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid mesylate
147059-75-4 C20H15F3N4O3.CH3SO3H=512.46
RT ≧99%(HPLC) 50 mM in water and to 100 mM in DMSO
517-91651 4187/10 UK 356618 10mg
Potent and selective inhibitor of MMP-3 (IC50 = 5.9 nM). Displays selectivity over a range of MMPs (IC50 values are 73, 840, 1790, 1900 and 51000 for MMP-13, MMP-9, MMP-2, MMP-14 and MMP-1 respectively).

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N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine
230961-08-7 C34H43N3O4=557.72
-20℃ ≧95%(HPLC) 100 mM in DMSO
514-91661 4188/1 UK 383367 1mg
- 4188/10 10mg
Potent and selective inhibitor of BMP-1 (procollagen C-proteinase; PCP) (IC50 = 44 nM). Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).

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3-(Aminocarbonyl)-β-(3-cyclohexylpropyl)-N-hydroxy-1,2,4-oxadiazole-5-propanamide
348622-88-8 C15H24N4O4=324.38
-20℃ ≧99%(HPLC) 100 mM in DMSO
- 4186/10 UK 5099 10mg
- 4186/50 50mg
Inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC).

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2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoic acid
56396-35-1 C18H12N2O2=288.3
4℃ ≧99%(HPLC) 100 mM in DMSO
518-92161 4206/10 Valdecoxib 10mg
- 4206/50 50mg
Selective and potent COX-2 inhibitor (in vitro IC50 values are 0.005 and 140 µM for human recombinant COX-2 and COX-1 respectively). Displays potent anti-inflammatory activity in vivo.

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4-(5-Methyl-3-phenylisoxazol-4-yl)benzenesulfonamide
181695-72-7 C16H14N2O3S=314.36
RT ≧99%(HPLC) 100 mM in DMSO
515-85961 3754/10 Varenicline tartrate 10mg
- 3754/50 50mg
Orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.

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7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
375815-87-5 C13H13N3.C4H6O6=361.37
RT ≧99%(HPLC) 100 mM in water and to 50 mM in DMSO
513-94311 3787/10 Viomycin 10mg
Member of the tuberactinomycin family of antibiotics. Inhibits group I intron splicing and prokaryotic protein synthesis. Freezes bacterial ribosomes in either the pre- or post-translational state. Facilitates trans-cleavage of the Neurospora VS ribozyme.

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(S)-3,6-Diamino-N-((3S,9S,12S,15S,Z)3((2R,4S)-6-amino-4-hydroxy-1,2,3,4-tetrahydropyridin-2-yl)-9,12-bis(hydroxymethyl)-2,5,8,11,14-pentaoxo-6-(ureidomethylene)-1,4,7,10,13-pentaazacyclohexadecan-15-yl)hexanamide disulfate
32988-50-4 C25H43N13O10.2H2SO4=881.85
-20℃ - 75 mM in water
518-86051 3760/10 Voriconazole 10mg
- 3760/50 50mg
Triazole antifungal agent. Displays potent activity against Candida, Cryptococcus and Aspergillus species.

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(2R,3S)-2-(2,4-Difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)-1-((1H)-1,2,4-triazol-1-yl)-butan-2-ol
137234-62-9 C16H14F3N5O=349.31
4℃ ≧99%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 5589/10 WAY 181187 oxalate 10mg
- 5589/50 50mg
High affinity and selective 5-HT6 agonist (Ki = 2.2 nM). Displays 60-fold selectivity over other 5-HT and monoamine receptors. Increases firing rate of 5-HT neurons. Modifies sleep and wakefulness profiles following direct injections into the dorsal raphe nucleus, in vivo. Orally bioavailable.

way-181187-oxalate_5589.png

1-[(6-Chloroimidazo[2,1-b]thiazol-5-yl)sulfonyl]-1H-indole-3-ethanamine oxalate
- C15H13ClN4O2S2.C2H2O4=470.91
RT ≧98%(HPLC) 100 mM in DMSO
515-91571 3890/10 WAY 207024 dihydrochloride 10mg
Gonadotropin releasing hormone receptor (GnRH-R) antagonist. Exhibits potent affinity (IC50 values are 12 and 71 nM for human and rat GnRH receptors respectively). Lowers plasma leuteinizing hormone levels in the rat. Orally active.

way-207024-dihydrochloride_3890.png

6-[[4-[2-[4-(1,1-Dimethylethyl)phenyl]-1H-benzimidazol-7-yl]-i-piperazinyl]methyl]-quinoxaline dihydrochloride
872002-73-8 C30H32N6.2HCl=549.54
RT ≧99%(HPLC) 85 mM in DMSO
512-91581 3904/10 WAY 208466 dihydrochloride 10mg
High affinity, selective 5-HT6 agonist (EC50 = 7.3 nM at the human 5-HT6 receptor). Elevates cortical GABA levels in vivo in rat frontal cortex. Exhibits antidepressant and anxiolytic-like effects.

way-208466-dihydrochloride_3904.png

3-[(-3-Fluorophenyl)sulfonyl]-N,N-dimethyl-1H-pyrrolo[2,3-b]pyridine-1-ethanamine dihydrochloride
1207064-61-6 C17H18FN3O2S.2HCl=420.33
RT ≧99%(HPLC) 80 mM in water and to 80 mM in DMSO
- 5951/10 WAY 252623 10mg
- 5951/50 50mg
Potent LXR agonist (IC50 values are 24 and 179 nM for LXRβ and LXRα, respectively). Reduces total serum cholesterol and LDL cholesterol, and inhibits lesion growth in models of atherosclerosis. Increases ABCA1 and ABCG1 mRNA levels in rat peripheral blood cells. Orally bioavailable.

way-252623_5951.png

2-[(2-Chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole
875787-07-8 C21H12ClF5N2=422.78
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
519-91591 3933/10 WAY 267464 dihydrochloride 10mg
Potent, selective non-peptide oxytocin receptor (OTR) agonist (Ki = 58.4 nM at human OTR). Exhibits anxiolytic-like effects. May have therapeutic potential for the treatment of psychosis and schizophrenia.

way-267464-dihydrochloride_3933.png

N-[[4-[(4,10-Dihydro-1-methylpyrazolo[3,4-b][1,5]benzodiazepin-5(1H)-yl)carbonyl]-2-methylphenyl]methyl]-4-[(3,5-dihydroxyphenyl)methyl]-1-piperazinecarboxamide dihydrochloride
1432043-31-6 C32H35N7O4.2HCl=654.59
-20℃ ≧97%(HPLC) 80 mM in DMSO and to 5 mM in water
512-91721 4194/10 WY 45233 succinate 10mg
- 4194/50 50mg
Serotonin and noradrenalin reuptake inhibitor (SNRI); selective for human serotonin (SERT) and noradrenalin (NET) transporters against 96 other targets (Ki values are 40.2 and 558.4 nM for SERT and NET respectively). Inhibits [3H]5-HT and [3H]NE uptake (IC50 values are 47.3 and 531.3 nM). Salt form of the major active metabolite of venlafaxine (Cat. No. 2917).

wy-45233-succinate_4194.png

4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol succinate
448904-47-0 C16H25NO2.C4H6O4=381.46
4℃ ≧99%(HPLC) 50 mM in water and to 100 mM in DMSO
556-02311 4282/10 WYE 687 dihydrochloride 10mg
- 4282/50 50mg
Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) (IC50 = 7 nM). Displays selectivity for mTOR over PI 3-Kα (〜100-fold) and PI 3-Kγ (〜500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1α expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis.

wye-687-dihydrochloride_4282.png

N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-carbamic acid methyl ester hydrochloride
1062161-90-3 C28H32N8O3=601.53
RT ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
514-64051 3085/10 Ziprasidone hydrochloride 10mg
- 3085/50 50mg
Atypical antipsychotic that displays combined serotonin and dopamine receptor antagonism. Displays high affinity at 5-HT2A receptors with a 5-HT2A/D2 affinity ratio greater than any other clinically available atypical antipsychotics (pKi values are 9.38, 8.88, 8.69, 8.47, 8.32, 8.14, 7.98, 7.49, 7.33 and 6.28 for 5-HT2A, 5-HT2C, 5-HT1D, 5-HT1A, D2, D3, α1, D4, H1 and D1 receptors respectively).

ziprasidone-hydrochloride_3085.png

5-[2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride
138982-67-9 C21H21ClN4OS.HCl=449.4
RT ≧99%(HPLC) 10 mM in DMSO
558-04691 2727/10 Zoniporide dihydrochloride 10mg
- 2727/50 50mg
Sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor that displays selectivity over other NHE isoforms (Ki values are 14, 2200 and 220000 nM for human NHE1, human NHE2 and rat NHE3 respectively). Inhibits NHE1 dependent 22Na+ uptake in vitro (IC50 = 14 nM) and provides cardioprotection from myocardial ischemic injury in vivo (EC50 = 0.25 nM). Also inhibits MMP2/9 activity and invasion in breast cancer cells.

zoniporide-dihydrochloride_2727.png

[1-(Quinolin-5-yl)-5-cyclopropyl-1H-pyrazole-4-carbonyl]guanidine dihydrochloride
241799-10-0 C17H16N6O.2HCl=393.27
-20℃ ≧99%(HPLC) 10 mM in water and to 100 mM in DMSO
 

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