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Tocris社
AstraZeneca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。
アストラゼネカ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
511-20861 1276/10 AG 1478 hydrochloride 10mg
- 1276/50 50mg
Potent and selective inhibitor of epidermal growth factor receptor kinase (IC50 values 3 nM for EGFR and > 100 µM for ErbB2 and PDGFR). Inhibits proliferation of NCI-H2170 NSCLC cells in vitro (IC50 = 1 µM).
N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinanine hydrochloride
170449-18-0 C16H14ClN3O2.HCl=352.22
-20℃ ≧98%(HPLC) 10 mM in DMSO with gentle warming
515-80841 3388/10 Anastrozole 10mg
511-80843 3388/50 50mg
Potent and highly selective aromatase (CYP19) inhibitor (IC50 = 15 nM) that has no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo. Orally active.
※ライセンス保持者との契約により販売量制限がございます。1ユーザーあたり1g/年以上購入はできません。
α1,α1,α3,α3-Tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-benzenediacetonitrile
120511-73-1 C17H19N5=293.37
RT ≧99%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
513-88201 3966/10 AR-A 014418 10mg
- 3966/50 50mg
Selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 µM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.
N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea
487021-52-3 C12H12N4O4S=308.31
4℃ ≧99%(HPLC) 100 mM in DMSO and to 5 mM in ethanol
515-94371 3969/10 AR-C 102222 10mg
- 3969/50 50mg
Inducible nitric oxide synthase (iNOS) inhibitor; selective for iNOS over eNOS (IC50 values are 0.037 and >100 µM for iNOS and eNOS respectively). Exhibits antinociceptive and anti-inflammatory activity in rodent pain models.
5-[(4'-Amino-5',8'-difluorospiro[piperidine-4,2'(1'H)-quinaxolin]-1-yl)carbonyl]-2-pyridinecarbonitrile hydrochloride
253771-21-0 C19H16F2N6O.HCl=418.83
4℃ ≧98%(HPLC) 25 mM in water and to 100 mM in DMSO
- 4960/1 AR-C155858 1mg
Inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively). Exhibits no activity at MCT4. Blocks proliferation of Raji lymphoma cells in vitro. Inhibits glycolysis and glutathione synthesis in cancer cells.
6-[(3,5-Dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
496791-37-8 C21H27N5O5S=461.53
-20℃ ≧98%(HPLC) 100 mM in DMSO
518-92921 3321/1 AR-C 66096 tetrasodium salt 1mg
Potent and selective P2Y12 receptor antagonist. Blocks ADP-induced inhibition of adenylyl cyclase in vitro (pKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).
2-(Propylthio)adenosine-5'-O-(β,γ-difluoromethylene)triphosphate tetrasodium salt
145782-74-7 C14H18F2N5Na4O12P3S=703.26
-20℃ ≧98%(HPLC) water (supplied pre-dissolved at a concentration of 10mM)
517-93851 3319/10 ARL 17477 dihydrochloride 10mg
- 3319/50 50mg
Selective neuronal nitrogen oxide synthase (nNOS) inhibitor (IC50 values are 1 and 17 µM for nNOS and endothelial NOS respectively). Reduces ischemic cell damage after middle cerebral artery (MCA) occlusion in rats. Displays a synergistic neuroprotective effect when combined with either an NMDA or AMPA receptor antagonist.
N-[4-[2-[[(3-Chlorophenyl)methyl]amino]ethyl]phenyl]-2-thiophenecarboxamide dihydrochloride
866914-87-6 C20H20ClN3S.2HCl=442.83
RT ≧99%(HPLC) 50 mM in water and to 100 mM in DMSO
518-93881 3964/10 AR-R 17779 hydrochloride 10mg
Selective agonist of α7 nAChRs (Ki values are 190 and 16000 nM for rat α7 and α4β2 receptors respectively). CNS penetrant after systemic administration.
(3S)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidine]-2'-one hydrochloride
178419-42-6 C9H14N2O2.HCl=218.68
RT - 50 mM in DMSO and to 100 mM in water
- 2172/10 AZ 10417808 10mg
- 2172/50 50mg
Selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 µM). Completely blocks staurosporine-induced intracellular DEVDase activity in SH-SY5Y cells (IC50 = 14.9 µM).
2-[(3,4-Dichlorophenyl)amino]-1,4-dihydro-6-nitro-4-oxo-N-2-propenyl-8-quinazolinecarboxamide
331645-84-2 C18H13Cl2N5O4=434.23
RT ≧98%(HPLC) 25 mM in DMSO
514-93861 3323/10 AZ 10606120 dihydrochloride 10mg
- 3323/50 50mg
Potent P2X7 receptor antagonist (KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively). Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator. Inhibits tumor growth and displays antiangiogenic effects in mice.
N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride
607378-18-7 C25H34N4O2.2HCl=495.48
RT ≧98%(HPLC) 25 mM in water and to 100 mM in DMSO
513-93831 3317/10 AZ 11645373 10mg
- 3317/50 50mg
Potent and selective human P2X7 antagonist (KB values are 5 - 7 and > 10,000 nM at hP2X7 and rP2X7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro (KB values are 15 and 92 nM respectively).
3-[1-[[(3'-Nitro[1,1'-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione
227088-94-0 C24H21N3O5S=463.51
4℃ ≧98%(HPLC) 10 mM in DMSO
- 4838/10 AZ 12080282 dihydrochloride 10mg
- 4838/50 50mg
Inhibitor of Hedgehog (Hh) signaling (IC50 <0.012 µM in a firefly reporter assay against the Hh pathway). Shown to displace cyclopamine in HeLa cells expressing Smoothened. Exhibits selectivity against p38α. Orally bioavailable.
N-[5-(1H-Imidazol-2-yl)-2-methylphenyl]-4-(2-pyridinylmethoxy)benzamide dihydrochloride
- C23H20N4O2.2HCl=457.35
RT ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
- 5198/10 AZ 20 10mg
- 5198/50 50mg
Potent and selective ATR kinase inhibitor (IC50 = 5 nM). Exhibits 7.6-fold selectivity over mTOR and selectivity over a panel of 442 kinases, including ATM kinase, PI3-K isoforms, and DNA-PK. Inhibits cell growth in cell lines with high baseline levels of replication stress. Displays antitumor effects in vivo.
4-[4-[(3R)-3-Methyl-4-morpholinyl]-6-[1-(methylsulfonyl)cyclopropyl]-2-pyrimidinyl]-1H-indole
1233339-22-4 C21H24N4O3S=412.51
-20℃ ≧98%(HPLC) 50 mM in DMSO and to 10 mM in ethanol
512-93921 3994/10 AZ 3146 10mg
- 3994/50 50mg
Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). Displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. Interferes with chromosome alignment and overrides spindle assembly checkpoint. Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.
9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
1124329-14-1 C24H32N6O3=452.55
4℃ ≧99%(HPLC) 25 mM in DMSO and to 75 mM in ethanol
- 4836/10 AZ 628 10mg
- 4836/50 50mg
Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases; inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide
878739-06-1 C27H25N5O2=451.52
4℃ ≧98%(HPLC) 100 mM in DMSO
- 4837/10 AZD 3988 10mg
- 4837/50 50mg
Potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, KV11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
trans-4-[-[[[5-[(3,4-Difluorophenyl)amino]-1,3,4-oxadiazol-2-yl]carbonyl]amino]phenyl]cyclohexaneacetic acid
892489-52-0 C23H22F2N4O4=456.44
4℃ ≧98%(HPLC) 100 mM in DMSO and to 10 mM in 1eq. NaOH with gentle warming
515-93911 3968/10 AZD 5438 10mg
- 3968/50 50mg
Potent inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9 (IC50 values are 16, 6 and 20 nM respectively). Exhibits antiproliferative activity in human tumor cell lines. Blocks cell cycling at G2-M, S and G1 phases; reduces the proportion of actively cycling cells in vivo.
4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
602306-29-6 C18H21N5O2S=371.46
RT ≧99%(HPLC) 100 mM in DMSO
- 5141/10 AZD 5582 dihydrochloride 10mg
- 5141/50 50mg
Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice.
3,3'-[2,4-Hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolinamide
- C58H78N8O8.2HCl=1088.21
-20℃ ≧97%(HPLC) 100 mM in water and to 100 mM in DMSO
- 4839/10 AZD 6482 10mg
- 4839/50 50mg
Potent and selective inhibitor of PI 3-kinase β (PI 3-Kβ) (IC50 values are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, respectively). Selectively inhibits in vivo growth of the PTEN-deficient tumor xenografts HCC70 and PC3. Also exhibits antithrombotic activity.
(-)-2-[[(1R)-1-[7-Methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid
1173900-33-8 C22H24N4O4=408.45
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 10 mM in 1eq. HCl
- 5199/10 AZD 7762 hydrochloride 10mg
- 5199/50 50mg
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50 vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents. Active in vivo.
3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-thiophenecarboxamide hydrochloride
1246094-78-9 C17H19FN4O2S.HCl=398.88
-20℃ ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
511-93871 3963/10 AZM 475271 10mg
- 3963/50 50mg
Src tyrosine kinase inhibitor. Reduces tumor size, vascularity and metastasis, and increases apoptosis in human pancreatic cells grown in nude mice. Also exhibits antiangiogenic activity in vitro and in vivo. Sensitizes tumor cells to the cytotoxic effects of gemcitabine (Cat. No. 3259).
N-(2-Chloro-5-methoxyphenyl)-6-methoxy
476159-98-5 C23H27ClN4O3=442.94
RT ≧99%(HPLC) 100 mM in DMSO
512-80851 3389/10 Bicalutamide 10mg
518-80853 3389/50 50mg
Orally active non-steroidal androgen receptor antagonist (IC50 = 190 nM). Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.
※ライセンス保持者との契約により販売量制限がございます。1ユーザーあたり1g/年以上購入はできません。
N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
90357-06-5 C18H14F4N2O4S=430.37
RT ≧99%(HPLC) 100 mM in DMSO and to 10 mM in ethanol
518-93901 3967/10 GPi 688 10mg
- 3967/50 50mg
Allosteric glycogen phosphorylase inhibitor; acts at the indole site of glycogen phosphorylase. Inhibits glucagon-mediated hyperglycemia in vivo in the rat.
2-Chloro-N-[1-[(2R)-2,3-dihydroxypropyl]-1,2,3,4-tetrahydro-2-oxo-3-quinolinyl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
918902-32-6 C19H18ClN3O4S=419.88
4℃ ≧99%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
537-58031 0821/10 ICI 118,551 hydrochloride 10mg
- 0821/50 50mg
Very selective β2 adrenergic antagonist/inverse agonist (Ki values are 1.2, 120 and 257 nM for β2, β1 and β3 receptors respectively). Active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
(±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride
72795-01-8 C17H27NO2.HCl=313.87
RT ≧98%(HPLC) 10 mM in DMSO and to 10 mM in water
- 0827/1 ICI 154,129 1mg
Selective δ opioid antagonist.
-
83420-94-4 C34H46N4O6S=638.83
-20℃ - 1 mg/ml in methanol
- 0833/50 ICI 162,846 50mg
A potent histamine H2 receptor antagonist.
N-[1-(4-Carboxamidobutyl)-1H-pyrazol-3-yl)]-N'-(2,2,2-trifluoroethyl)guanidine
84545-30-2 C11H17F3N6O=306.29
RT - ethanol and to 100 mM in DMSO
- 0820/1 ICI 174,864 1mg
- 0820/5 5mg
Selective δ opioid antagonist. Exhibits partial agonist in vitro activity at δ receptors at high concentrations.
-
89352-67-0 C38H53N5O7=691.87
-20℃ - 69.19 mg/ml in DMSO and to 1 mg/ml in water
- 0836/10 ICI 185,282 10mg
- 0836/50 50mg
Potent thromboxane receptor antagonist.
5-(Z)-7-(4-o-Hydroxyphenyl-2-trifluoromethyl-1,3 dioxan-cis-5-yl)heptenoic acid
106393-80-0 C18H21F3O5=374.36
-20℃ - DMSO
- 0837/10 ICI 192,605 10mg
- 0837/50 50mg
Potent thromboxane A2 receptor (TP receptor) antagonist. Competitively inhibits contractile responses to U 46619 (Cat. No. 1932).
4-(Z)-6-(2-o-Chlorophenyl-4-o-hydroxyphenyl-1,3-dioxan-cis-5-yl)hexenoic acid
117621-64-4 C22H23ClO5=402.87
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 0778/10 ICI 199,441 hydrochloride 10mg
- 0778/50 50mg
Highly potent κ agonist, 146-fold more active than U-50488 (Cat. No. 0495) in vitro.
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl]acetamide hydrochloride
115199-84-3 C21H24Cl2N2O.HCl=427.8
RT ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
- 0822/10 ICI 204,448 hydrochloride 10mg
- 0822/50 50mg
Peripherally acting κ agonist.
(RS)-[3-[1-[[(3,4-Dichlorophenyl)acetyl]methylamino]-2-(1-pyrrolidinyl)ethyl]phenoxy]acetic acid hydrochloride
121264-04-8 C23H26Cl2N2O4.HCl=501.84
RT ≧98%(HPLC) 100 mM in DMSO
- 0832/10 ICI 89406 10mg
- 0832/50 50mg
β-adrenergic antagonist and low efficacy partial agonist; does not affect resting cardiac parameters.
N-[2-[3-(2-Cyanophenoxy)-2-hydroxypropylamino]ethyl]-N'-phenylurea
53671-71-9 C19H22N4O3=354.41
RT ≧99%(HPLC) ethanol and to 100 mM in DMSO
512-58883 3000/10 Iressa 10mg
516-58881 3000/50 50mg
Orally active, selective inhibitor of EGFR tyrosine kinase (IC50 = 23 - 79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts.
※ライセンス保持者との契約により販売量制限がございます。1ユーザーあたり1g/年以上購入はできません。
N-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
184475-35-2 C22H24ClFN4O3=446.9
RT ≧98%(HPLC) 100 mM in DMSO and to 10 mM in ethanol
- 4176/5 KU 60019 5mg
- 4176/25 25mg
Potent ATM kinase inhibitor (IC50 = 6.3 nM). Exhibits little to no nonspecific target effects against a panel of 229 protein kinases; displays similar target selectivity to KU 55933 (Cat. No. 3544). Inhibits migration and invasion of human glioma cells in vitro.
(2R,6S-rel)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl-4-morpholineacetamide
925701-46-8 C30H33N3O5S=547.67
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
516-93821 3282/10 NAD 299 hydrochloride 10mg
- 3282/50 50mg
Selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro). Enhances the action of selective 5-HT reuptake inhibitors and reverses citalopram-induced (Cat. No. 1427) inhibition of serotonergic cell firing.
(3R)-3-(Dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrochloride
184674-99-5 C18H23FN2O2.HCl=354.85
RT ≧98%(HPLC) 100 mM in water and to 100 mM in DMSO
584-97143 1037/10 PD 153035 hydrochloride 10mg
- 1037/50 50mg
An extremely potent inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase, with an IC50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations.
4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline hydrochloride
183322-45-4 C16H14BrN3O2.HCl=396.67
RT - 10 mM in DMSO with gentle warming
- 1380/10 PMPA (NAALADase inhibitor) 10mg
- 1380/50 50mg
Highly potent and selective inhibitor of glutamate carboxypeptidase 2 (GCP II/N-acetylated α-linked dipeptidase/NAALADase) with a Ki value of 275 pM. Neuroprotective; protects against glutamate-mediated motor neuron degeneration and reduces volume of injury following middle cerebral artery occlusion (MCAO).
2-(Phosphonomethyl)pentane-1,5-dioic acid
173039-10-6 C6H11O7P=226.12
RT - 100 mM in water
- 0829/100 Pronethalol hydrochloride 100mg
β-adrenergic antagonist, clinically effective in the treatment of angina pectoris and some arrhythmias.
2-Isopropylamino-1-(2-naphthyl)ethanol hydrochloride
51-02-5 C15H19NO.HCl=265.78
RT ≧99%(HPLC) 100 mM in water
- 1622/10 Remacemide hydrochloride 10mg
- 1622/50 50mg
Non-competitive NMDA receptor antagonist; blocks ion channel and allosteric modulatory site (IC50 = 8 - 68 mM). Anticonvulsant in vivo and metabolizes to a more potent desglycine analog. Weakly blocks voltage-dependent Na+ channels (IC50 = 161 mM).
2-Amino-N-(1-methyl-1,2-diphenylethyl)acetamide hydrochloride
111686-79-4 C17H20N2O.HCl=304.82
RT ≧99%(HPLC) 100 mM in water
510-93841 3318/10 SC 514 10mg
516-93843 3318/50 50mg
Orally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 µM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 µM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.
4-Amino-[2',3'-bithiophene]-5-carboxamide
354812-17-2 C9H8N2OS2=224.3
4℃ ≧98%(HPLC) 100 mM in DMSO and to 10 mM in ethanol
- 0999/100 Tamoxifen citrate 100mg
Estrogen receptor antagonist/partial agonist. Selective and potent inhibitor of mammalian sterol isomerase. Neuroprotective in female rats in vivo. Also high affinity agonist at the membrane estrogen receptor GPER.
(Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine citrate
54965-24-1 C26H29NO.C6H8O7=563.65
RT ≧99%(HPLC) 5 mM in ethanol with gentle warming and to 100 mM in DMSO
515-93891 3965/10 Tesaglitazar 10mg
- 3965/50 50mg
Dual-specificity PPARα/γ agonist (IC50 values are 0.35 and 3.8 µM for PPARγ and PPARα respectively). Prevents atherosclerosis progression in E3L.CETP transgenic mice. Also reduces insulin resistance in obese Zucker rats. Orally active.
(S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
251565-85-2 C20H24O7S=408.47
RT ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
578-98701 0826/10 Tiotidine 10mg
- 0826/50 50mg
Potent histamine H2-receptor antagonist with negligible activity against H1- and H3- receptors.
-
69014-14-8 C10H16N8S2=312.41
RT ≧99%(HPLC) 10 mM in ethanol and to 100 mM in DMSO
515-92791 0950/10 Xamoterol hemifumarate 10mg
- 0950/50 50mg
β1-adrenoceptor-selective partial agonist (pA2 values are 7.4 - 7.8 and 5.2 - 6.2 at β1- and β2-adrenoceptors respectively).
1-(4-Hydroxyphenoxy)-3-[2-(4-morpholinocarboxamido)ethylamino]-2-propanol hemifumarate
73210-73-8 C16H25N3O5.0.5C4H4O4=397.43
RT ≧97%(HPLC) 50 mM in water and to 100 mM in DMSO
- 2154/10 ZD 2079 10mg
- 2154/50 50mg
β3-adrenoceptor agonist. Relaxes rat mesenteric artery and isolated aorta in vitro. Inhibits ob gene expression and circulating leptin levels in lean mice in vivo.
4-[2-[[(2R)-2-Hydroxy-2-phenylethyl]amino]ethoxy]-benzeneacetic acid hydrochloride
178600-17-4 C18H21NO4.HCl=351.83
4℃ ≧99%(HPLC) 25 mM in water
521-44983 0930/10 ZD 7114 hydrochloride 10mg
- 0930/50 50mg
β3-adrenoceptor agonist. Active metabolite ICI 215,001 hydrochloride (Cat. No. 0929) also available.
(S)-4-[2-Hydroxy-3-phenoxypropylaminoethoxy]-N-(2-methoxyethyl)phenoxyacetamide hydrochloride
129689-28-7 C22H30N2O6.HCl=454.95
RT - 100 mM in DMSO
523-85681 1211/10 ZD 7155 hydrochloride 10mg
529-85683 1211/50 50mg
A potent and selective competitive antagonist for the angiotensin II type 1 (AT1) receptor. Displaces [125I]-angiotensin II binding with an IC50 value of 3.8 nM in guinea pig adrenal gland membranes. Orally active, and is more potent and longer-acting than the prototype AT1 antagonist, losartan.
5,7-Diethyl-3,4-dihydro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,6-naphthyridin-2(1H)-one hydrochloride
146709-78-6 C26H26N6O.HCl=474.99
4℃ ≧98%(HPLC) 10 mM in water with gentle warming
575-25561 1000/10 ZD 7288 10mg
571-25563 1000/50 50mg
Sino-atrial node function modulator; blocks the hyperpolarization activated cation current If (HCN channel). Blocks Ih in central neurons. Increases NMDA-evoked noradrenalin release in rat brain in vitro.
4-Ethylphenylamino-1,2-dimethyl-6-methylaminopyrimidinium chloride
133059-99-1 C15H21ClN4=292.81
4℃ ≧99%(HPLC) 100 mM in water and to 100 mM in DMSO
- 3322/10 ZD 9379 10mg
NMDA receptor antagonist; acts at glycine site. Neuroprotective; reduces infarct size and frequency of spreading depressions in a rat model of ischemic stroke. Brain penetrant.
7-Chloro-2,3-dihydro-2-(4-methoxy-2-methylphenyl)pyridazino [4,5-b] quinoline-1,4,10(5H)trione
170142-20-8 C19H14ClN3O4=383.79
4℃ ≧98%(HPLC) 50 mM in DMSO and to 20 mM in 1eq. NaOH
- 0882/10 ZM 226600 10mg
- 0882/50 50mg
Potent Kir6 (KATP) channel opener (EC50 = 0.5 µM), devoid of antiandrogen properties.
N-(4-Phenylsulfonylphenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
147695-92-9 C16H14F3NO4S=373.35
RT - 100 mM in DMSO
507-37871 1036/10 ZM 241385 10mg
503-37873 1036/50 50mg
Potent and highly selective A2A adenosine antagonist, with a pA2 of 9.02 for A2A receptors in guinea pig cardiac vasculature and selectivities of 1000, 91 and 500,000 over A1, A2B and A3 sites respectively. Active in vivo.
4-(2-[7-Amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol
139180-30-6 C16H15N7O2=337.34
RT ≧99%(HPLC) 5 mM in ethanol and to 100 mM in DMSO
- 2499/1 ZM 306416 hydrochloride 1mg
- 2499/10 10mg
Inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. Inhibits activity of KDR and FLT VEGF receptors (IC50 values are 100 nM and 2 µM respectively) and displays > 3-fold selectivity over FGFR-1. Orally active in vivo.
4-[(4'-Chloro-2'-fluoro)phenylamino]-6,7-dimethoxyquinazoline hydrochloride
196603-47-1 C16H13N3O2FCl.HCl=370.21
RT ≧99%(HPLC) 10 mM in DMSO
- 2475/1 ZM 323881 hydrochloride 1mg
- 2475/10 10mg
Potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) activity. Selectively inhibits VEGFR-2 (IC50 = 2 nM) over VEGFR-1 and a range of other receptor tyrosine kinases such as PDGFRβ, FGFR1, EGFR and erbB2 (IC50 > 50 µM). Inhibits VEGF-A-induced endothelial cell proliferation in vitro (IC50 = 8 nM).
5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride
193000-39-4 C22H18FN3O2.HCl=411.86
4℃ ≧99%(HPLC) 50 mM in DMSO
- 1321/10 ZM 336372 10mg
- 1321/50 50mg
Potent, selective inhibitor of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf). Shows 10-fold selectivity over B-Raf. Also inhibits SAPK2/p38 (IC50 = 2 µM). Selective over 17 other protein kinases including PKA, PKC, p42 MAPK, CDK1 and SAPK1/JNK (up to 50 µM). Also available as part of the MAPK Cascade Inhibitor Tocriset™.
3-(Dimethylamino)-N-[3-[(4-hydroxybenzoyl)-amino]-4-methylphenyl]benzamide
208260-29-1 C23H23N3O3=389.45
4℃ ≧99%(HPLC) 100 mM in DMSO
572-36181 1367/10 ZM 39923 hydrochloride 10mg
- 1367/50 50mg
Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3). pIC50 values are 7.1, 5.6, 4.4, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively. Breaks down in neutral buffer (t1/2 = 36 mins, pH 7.43, 25°C) to form ZM 449829 (Cat. No. 1366).
3-benzylisopropylamino-1-naphthalen-2-yl-propan-1-one hydrochloride
58753-54-1 C23H25NO.HCl=367.92
4℃ ≧99%(HPLC) 100 mM in DMSO
510-24471 2458/10 ZM 447439 10mg
Novel, selective ATP-competitive inhibitor of Aurora B kinase in vitro (IC50 values are 50, 250 and 1000 nM for Aurora B, C and A kinases respectively). Selective over a range of other kinases including cdk1 and PLK1 (IC50 > 10 µM). Inhibits cell division and displays selective toxicity towards proliferating tumor cells versus non-dividing cells.
N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
331771-20-1 C29H31N5O4=513.59
-20℃ ≧98%(HPLC) 100 mM in DMSO
572-36061 1366/10 ZM 449829 10mg
- 1366/50 50mg
Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) which binds competitively to the JAK3 ATP site. pIC50 values are 6.8, 5.0, 4.7, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively. Inhibits STAT-5 phosphorylation and T cell proliferation.
1-(2-Naphthalenyl)-2-propen-1-one
4452-06-6 C13H10O=182.22
-20℃ ≧98%(HPLC) 100 mM in DMSO

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