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Tocris社
GlaxoSmithKline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。
グラクソスミスクライン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
- 5256/10 AH 7614 10mg
- 5256/50 50mg
Selective free fatty acid receptor 4 (FFA4/GPR120) antagonist (pIC50 values are 7.1 and < 4.6 for human FFA4 and FFA1 receptors respectively). inhibits linoleic acid and GSK 137647A-induced intracellular calcium accumulation in U2OS osteosarcoma cells expressing the FFA4 receptor.
4-Methyl-N-9H-xanthen-9-yl-benzenesulfonamide
6326-06-3 C20H17NO3S=351.42
4℃ ≧98%(HPLC) 100 mM in DMSO
550-79241 1207/10 BRL 15572 hydrochloride 10mg
- 1207/50 50mg
A selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
3-[4-(4-Chlorophenyl)piperazin-1-yl]-1,1-diphenyl-2-propanol hydrochloride
1173022-77-9 C25H27ClN2O.HCl=443.42
4℃ - 10 mM in DMSO and to 50 mM in ethanol
522-44991 0948/10 BRL 37344, sodium salt 10mg
528-44993 0948/50 50mg
Potent and selective β3 adrenoceptor agonist (Ki values are 287, 1750 and 1120 nM for β3, β1 and β2 receptors respectively). Also available as part of the β-Adrenoceptor Agonist Tocriset™.
(R*,R*)-(±)-4-[2-[(2-(3-Chlorophenyl)-2-hydroxyethyl)amino]propyl]phenoxyacetic acid, sodium salt
127299-93-8 C19H21NO4ClNa=385.82
RT ≧98%(HPLC) 100 mM in water
501-38371 1133/10 BRL 44408 maleate 10mg
- 1133/50 50mg
Selective α2A-adrenoceptor antagonist (Ki = 1.7 nM and 144.5 nM at α2A and α2B-adrenergic receptors respectively). increases hippocampal noradrenalin release following systemic administration. Also available as part of the α2-Adrenoceptor Tocriset™.
2-[(4,5-Dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole maleate
681806-46-2 C13H17N3.C4H4O4=331.37
-20℃ ≧98%(HPLC) 100 mM in water
- 2237/10 BRL 50481 10mg
- 2237/50 50mg
Selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (Ki = 180 nM). Displays > 200-fold selectivity over PDE1B, PDE1C, PDE2, PDE3, PDE4A4 and PDE5.
N,N,2-Trimethyl-5-nitro-benzenesulfonamide
433695-36-4 C9H12N2O4S=244.26
4℃ ≧99%(HPLC) 100 mM in ethanol and to 100 mM in DMSO
- 0699/10 BRL 52537 hydrochloride 10mg
- 0699/50 50mg
The most κ/µ-selective and among the most potent κ ligands known (25 times more potent than morphine in vivo).
(±)-1-(3,4-Dichlorophenyl)acetyl-2-(1-pyrrolidinyl)methylpiperidine hydrochloride
112282-24-3 C18H24Cl2N2O.HCl=391.77
RT ≧98%(HPLC) 5 mM in water with gentle warming
- 1663/10 BW 373U86 10mg
Potent, selective non-peptide δ-opioid receptor agonist. Ki values are 1.8, 15 and 34 nM for δ, μ and κ receptors respectively. Centrally active following systemic administration in vivo.
4-[(αR*)-α-((2S*,5R*)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl]-N,N-diethylbenzamide
155836-50-3 C27H37N3O2=435.61
4℃ ≧99%(HPLC) 100 mM in 1eq. HCl
551-02741 4674/10 CZC 24832 10mg
- 4674/50 50mg
Selective inhibitor of PI 3-kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay). Exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins. Orally effective in a rodent model of inflammatory disease.
5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-3-pyridinesulfonamide
1159824-67-5 C15H17FN6O2S=364.4
4℃ ≧98%(HPLC) 100 mM in DMSO
516-80631 2902/10 D 4476 10mg
- 2902/50 50mg
Selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) that displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested. Suppresses site-specific phosphorylation and nuclear exclusion of FOXO1a.
4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
301836-43-1 C23H18N4O3=398.41
4℃ ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
557-02721 4646/10 Elacridar hydrochloride 10mg
P-glycoprotein (P-gp/ABCG1) inhibitor. Blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Also inhibits breast cancer resistance protein (BCRP/ABCG2). Orally active.
N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydrochloride
143851-98-3 C34H33N3O5.HCl=600.1
-20℃ ≧99%(HPLC) 20 mM in DMSO
514-29131 1659/10 Fenoldopam hydrochloride 10mg
- 1659/50 50mg
Selective D1-like dopamine receptor partial agonist (EC50 = 57 nM). Vasodilator in vivo and does not readily cross the blood-brain barrier. Also α2-adrenoceptor antagonist in vitro (Ki = 15 - 25 nM).
6-Chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol hydrochloride
181217-39-0 C16H16ClNO3.HCl=342.22
4℃ ≧98%(HPLC) 10 mM in water
554-75861 2007/10 Fluticasone propionate 10mg
- 2007/50 50mg
High affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM). Potently stimulates glucocorticoid receptor-mediated transactivation of gene expression and enhances human eosinophil apoptosis (EC50 = 3.7 nM) in vitro. inhibits mast cell accumulation in nasal mucosa following topical administration. Lipophilic anti-inflammatory agent with low oral bioavailability. Also potentiates KV1 channels (EC50 = 37 nM).
(6α,11β,16α,17α)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid fluoromethyl ester
80474-14-2 C25H31F3O5S=500.57
RT ≧98%(HPLC) 50 mM in DMSO
510-92361 2348/10 Gavestinel 10mg
- 2348/50 50mg
Highly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (Kd = 0.8 nM). Displays > 1000-fold selectivity over NMDA, AMPA and kainate binding sites. Orally bioavailable and active in vivo.
4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
153436-38-5 C18H11Cl2N2O3Na=397.19
RT ≧98%(HPLC) 40 mM in DMSO
- 3995/1 GI 254023X 1mg
Selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17. Blocks constitutive release of IL-6R, CX3CL1 and CXCL16 in cell-based cleavage experiments. inhibits calcium ionophore-induced betacellulin shedding in IMPE cells. Prevents E-cadherin cleavage in A549 cells. inhibits ADAM10 mediated neuronal outgrowth of dorsal root ganglion neurons in vitro.
(2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-2-[(1S)-1-(N-hydroxyformamido)ethyl]-5-phenylpentanamide
260264-93-5 C21H33N3O4=391.5
-20℃ ≧98%(HPLC) 20 mM in DMSO
577-71791 1322/10 GR 113808 10mg
- 1322/50 50mg
Potent, selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, and Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). Displays > 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
144625-51-4 C19H27N3O4S=393.5
RT ≧98%(HPLC) 25 mM in 1eq. HCl
513-31671 1658/10 GR 125487 sulfamate 10mg
- 1658/50 50mg
Potent and selective 5-HT4 receptor antagonist (Ki = 0.19 nM for porcine 5-HT4). Centrally active following systemic administration in vivo.
5-Fluoro-2-methoxy-[1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]-1H-indole-3-methylcarboxylate sulfamate
859502-43-5 C19H26FN3O5S.H2NSO3H=524.58
RT ≧97%(HPLC) 10 mM in water with gentle warming
516-32641 1274/10 GR 159897 10mg
- 1274/50 50mg
A potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.
5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
158848-32-9 C23H27FN2O2S=414.54
-20℃ ≧97%(HPLC) 50 mM in DMSO and to 10 mM in ethanol
539-50931 0864/10 GR 46611 10mg
- 0864/50 50mg
5-HT1D receptor agonist. Blockade of GR 46611-induced hypothermia in the guinea pig provides a useful model with which to study the potency and duration of action of centrally acting 5-HT1D receptor ligands.
3-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)acrylamide
185259-85-2 C23H27N3O2=377.49
RT - 50 mM in DMSO and to 10 mM in ethanol
573-98751 1054/10 GR 55562 dihydrochloride 10mg
- 1054/50 50mg
A selective competitive 5-HT1B (5-HT1Dβ) silent antagonist with pKB values of 7.3 and 6.3 for human cloned 5-HT1B and 5-HT1D receptors respectively and only weak binding at a number of other 5-HT subtypes.
3-[3-(Dimethylamino)propyl]-4-hydroxy-N-[4-(4-pyridinyl)phenyl]benzamide dihydrochloride
159533-25-2 C23H25N3O2.2HCl=448.39
4℃ ≧98%(HPLC) 100 mM in water
- 1668/1 GR 64349 1mg
Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.
-
137593-52-3 C42H68N10O11S=921.12
-20℃ 成績書参照 1 mg/ml in water
- 1669/1 GR 73632 1mg
Potent and selective tachykinin NK1 receptor agonist (EC50 = 2 nM in guinea pig vas deferens). Active in vivo.
-
133156-06-6 C40H59N7O6S=766.01
-20℃ 成績書参照 1 mg/ml in water
- 1957/10 GR 79236 10mg
- 1957/50 50mg
Adenosine A1 receptor agonist (Ki = 3.1 nM). Anticonvulsive in mice following systemic administration in vivo.
N-[(1S,2S)-2-Hydroxycyclopentyl]adenosine
124555-18-6 C15H21N5O5=351.36
4℃ ≧99%(HPLC) 100 mM in water
- 1670/1 GR 82334 1mg
Tachykinin NK1 receptor antagonist.
-
129623-01-4 C69H91N15O16=1386.57
-20℃ 成績書参照 1 mg/ml in water
- 1667/1 GR 94800 1mg
Potent and selective tachykinin NK2 receptor antagonist (pKB values are 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors respectively). Active in vivo.
-
141636-65-9 C49H61N9O8=904.08
-20℃ 成績書参照 4 mg/ml in ethanol
511-92411 4026/10 GSK 1059615 10mg
- 4026/50 50mg
Potent inhibitor of PI 3-kinase α (PI3Kα) (IC50 = 2 nM). inhibits proliferation in BT474 cells and attenuates MAPK signaling.
5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
958852-01-2 C18H11N3O2S=333.36
4℃ ≧98%(HPLC) 10 mM in DMSO
- 5110/10 GSK 1562590 hydrochloride 10mg
- 5110/50 50mg
High affinity and selective urotensin II (UT) receptor antagonist (pKi values are 9.14, 9.28, 9.34, 9.64 and 9.66 at monkey, human, mouse, cat and rat recombinant receptors respectively). Exhibits selectivity for UT receptors over a range of GPCRs, ion channels, enzymes and neurotransmitter transporters. Supresses human urotensin-II (hU-II)-induced contraction of isolated rat aorta in vitro and ex vivo. inhibits the hU-II-induced increase in mean blood pressure in vivo. Orally active.
N-[(1R)-1-[3'-(Aminocarbonyl)[1,1'-biphenyl]-4-yl]-2-(1-pyrrolidinyl)ethyl]-6,7-dichloro-2,3-dihydro-N-methyl-3-oxo-4H-1,4-benzoxazine-4-acetamide hydrochloride
1003878-07-6 C30H30Cl2N4O4.HCl=617.95
4℃ ≧98%(HPLC) 100 mM in DMSO
- 5111/10 GSK 1838705 10mg
- 5111/50 50mg
Potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC50 values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC50 = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro, and causes complete regression of ALK-dependent tumors in vivo. Orally bioavailable.
2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
1116235-97-2 C27H29FN8O3=532.57
-20℃ ≧98%(HPLC) 100 mM in DMSO
558-29351 5257/10 GSK 137647 10mg
- 5257/50 50mg
Potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits greater than or equal to100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3. Enhances glucose-stimulated insulin secretion in Min6 cells. induces intracellular calcium accumulation in U2OS cells; this activity is inhibited by AH 7614 (Cat. No. 5256).
4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
349085-82-1 C16H19NO3S=305.39
RT ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
- 5106/5 GSK 2193874 5mg
- 5106/25 25mg
Potent and selective TRPV4 antagonist (IC50 values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.
3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
1336960-13-4 C37H38BrF3N4O=691.62
4℃ ≧98%(HPLC) 20 mM in 1eq. HCl and to 50 mM in DMSO
- 5303/5 GSK 2194069 5mg
- 5303/25 25mg
Potent human fatty acid synthase (hFASN) inhibitor (IC50 = 7.7 nM); inhibits hFAS β-ketoacyl reductase activity. inhibits lipid synthesis and attenuates proliferation of A549 non-small-cell lung cancer cells (EC50 = 15 nM) in vitro.
4-[4-(5-Benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
1332331-08-4 C25H24N4O3=428.48
4℃ ≧99%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
517-96531 4143/10 GSK 2334470 10mg
513-96533 4143/50 50mg
Potent 3-phosphoinositide-dependent protein kinase (PDPK1) inhibitor (IC50 ~ 10 nM). Exhibits no effect on other kinases including Aurora, ROCK, p38 MAPK and PI 3-K. Suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in vitro; exhibits limited inhibitory effect on Akt activation. Delays melanomagenesis and metastasis in BrafV600E::Pten(-/-) mice.
(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
1227911-45-6 C25H34N8O=462.59
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
- 4629/5 GSK 2578215A 5mg
- 4629/25 25mg
Potent LRRK2 inhibitor (IC50 values are 8.9 and 10.1 nM for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). Displays selectivity for LRRK2 over a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.
5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
1285515-21-0 C24H18FN3O2=399.42
RT ≧99%(HPLC) 100 mM in DMSO
- 5107/10 GSK 2606414 10mg
- 5107/50 50mg
Potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable.
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone
1337531-36-8 C24H20F3N50=451.44
-20℃ ≧99%(HPLC) 100 mM in DMSO
513-96511 4009/10 GSK 269962 10mg
- 4009/50 50mg
Potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively). Displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM); lowers blood pressure in a rat model of hypertension.
N-[3-[[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]benzamide
850664-21-0 C29H30N8O5=570.6
4℃ ≧99%(HPLC) 100 mM in DMSO and to 10 mM in ethanol with gentle warming
- 5140/10 GSK 2830371 10mg
- 5140/50 50mg
Potent and selective allosteric inhibitor of Wip1 phosphatase (IC50 = 6 nM). Exhibits selectivity for Wip1 over 21 other phosphatases. increases phosphorylation of Wip1 substrates, including p53, Chk2, H2AX and ATM. Attenuates tumor cell growth in a variety of lymphoid cell lines. Also inhibits lymphoma xenograft growth in vivo. Orally bioavailable.
5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
1404456-53-6 C23H29ClN4O2S=461.02
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
550-31521 5189/10 GSK 2837808A 10mg
Potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively). inhibits lactate production in selected cancer cell lines. Reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells. inhibits proliferation and induces apoptosis in Snu398 cells. inhibits transcription of histone 2B (H2B) gene in HCT116 and NCM460 cells. Cell permeable.
3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid
1445879-21-9 C31H25F2N5O7S=649.62
-20℃ ≧98%(HPLC) 100 mM in DMSO
514-92401 3726/1 GSK 429286 1mg
- 3726/10 10mg
- 3726/50 50mg
Selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide
864082-47-3 C21H16F4N4O2=432.37
4℃ ≧97%(HPLC) 100 mM in DMSO and to 25 mM in ethanol
514-92381 3572/10 GSK 650394 10mg
- 3572/50 50mg
Serum- and glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC50 values are 62 and 103 nM for SGK1 and SGK2 respectively). Displays >30-fold selectivity over Akt and other related kinases. inhibits androgen-stimulated growth of LNCaP cells, a human prostate carcinoma cell line (IC50 ~ 1 muM).
2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoic acid
890842-28-1 C25H22N2O2=382.45
RT ≧97%(HPLC) 100 mM in DMSO
511-90353 4144/10 GSK 690693 10mg
515-90351 4144/50 50mg
ATP-competitive pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM of Akt1, 2 and 3 respectively). Also exhibits some inhibition for AMPK, PKA and PAK and PKC isoforms (IC50 < 100 nM). Displays antiproliferative and apoptotic effects in tumor cell lines.
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol
937174-76-0 C21H27N7O3=425.48
-20℃ ≧98%(HPLC) 50 mM in DMSO
518-92421 4116/10 GSK 9027 10mg
- 4116/50 50mg
Glucocorticoid receptor agonist (pIC50 = 8). inhibits production of the proinflammatory mediator IL-6 in vivo.
N-[4-[1-(4-Fluorophenyl)-1H-indazol-5-yl-3-(trifluoromethyl)phenyl]benzenesulfonamide
1229096-88-1 C27H19F4N3O2S=525.52
RT ≧98%(HPLC) 100 mM in DMSO
514-00451 2229/10 GW 0742 10mg
- 2229/50 50mg
Potent and highly selective PPARδ agonist. EC50 values are 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. Neuroprotective in rat cerebellar granule neuronal cultures after brief (12-hour) exposure but exhibits inherent toxicity after prolonged (48-hour) incubation. increases rate of fatty acid oxidation and protects against ischemia/reperfusion injury in neonatal and adult cardiomyocytes.
[4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]acetic acid
317318-84-6 C21H17F4NO3S2=471.49
4℃ ≧98%(HPLC) 50 mM in ethanol and to 100 mM in DMSO
511-00461 1664/10 GW 1929 hydrochloride 10mg
- 1664/50 50mg
Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo.
N-(2-Benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-L-tyrosine hydrochloride
1217466-21-1 C30H29N3O4.HCl=532.03
4℃ ≧98%(HPLC) 100 mM in ethanol with gentle warming and to 100 mM in water
518-96441 2474/1 GW 3965 hydrochloride 1mg
- 2474/10 10mg
Selective, orally active non-steroidal agonist for the liver X receptor (LXR). in cell-based reporter gene assays, acts as a full agonist of hLXRα and hLXRβ (EC50 values are 190 and 30 nM respectively). Reduces angiotensin II-mediated increases in blood pressure; up-regulates ABCA1 gene expression and raises circulating HDL levels. Displays potent antiatherogenic activity in mouse models of atherosclerosis.
3-[3-[[[2-Chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]benzeneacetic acid hydrochloride
405911-17-3 C33H31NO3ClF3.HCl=618.51
RT ≧98%(HPLC) 100 mM in DMSO and to 20 mM in ethanol
511-32691 2473/10 GW 4064 10mg
- 2473/50 50mg
Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 μM. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes.
3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid
278779-30-9 C28H22Cl3NO4=542.84
4℃ ≧97%(HPLC) 100 mM in DMSO and to 10 mM in ethanol
- 2238/10 GW 441756 10mg
- 2238/50 50mg
Potent, selective inhibitor of the NGF receptor tyrosine kinase A (TrkA) (IC50 = 2 nM). Displays > 100-fold selectivity over a range of other kinases.
1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one
504433-23-2 C17H13N3O=275.31
RT ≧99%(HPLC) 15 mM in DMSO
- 1381/10 GW 5074 10mg
- 1381/50 50mg
Potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM). Displays greater than or equal to 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.
3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
220904-83-6 C15H8Br2INO2=520.94
-20℃ ≧98%(HPLC) 1 mM in ethanol and to 100 mM in DMSO
512-20771 2239/10 GW 583340 dihydrochloride 10mg
- 2239/50 50mg
Potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). Selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μuM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μuM for inhibition of non-tumor cell line HFF). inhibits tumor growth in vivo by ~ 80% in a murine xenograft model following oral administration.
N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-4-quinazolinamine dihydrochloride
1173023-85-2 C28H25ClFN5O3S2.2HCl=671.03
4℃ ≧97%(HPLC) 100 mM in DMSO with gentle warming
- 4668/10 GW 627368 10mg
- 4668/50 50mg
Selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays). Affinity for all other prostanoid receptors is < 5.3. inhibits U-46619 induced human platelet aggregation.
4-(4-,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)benzeneacetamide
439288-66-1 C30H28N2O6S=544.62
-20℃ ≧98%(HPLC) 100 mM in DMSO
513-96751 4618/10 GW 6471 10mg
- 4618/50 50mg
PPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
N-((2S)-2-(((1Z)-1-Methyl-3-oxo-3-(4-(trifluoromethyl)phenyl)prop-1-enyl)amino)-3-(4-(2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy)phenyl)propyl)propanamide
880635-03-0 C35H36F3N3O4=619.67
4℃ ≧98%(HPLC) 75 mM in DMSO and to 20 mM in ethanol
515-00481 1677/10 GW 7647 10mg
- 1677/50 50mg
Potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro. Has lipid-lowering effects following oral administration in vivo. Reduces NO production in macrophages; exhibits anti-inflammatory properties.
2-[[4-[2-[[(Cyclohexylamino)carbonyl](4-cyclohexylbutyl)amino]ethyl]phenyl]thio]-2-methylpropanoic acid
265129-71-3 C29H46N2O3S=502.75
RT ≧99%(HPLC) 25 mM in ethanol and to 100 mM in DMSO
519-96471 3264/10 GW 788388 10mg
- 3264/50 50mg
Potent inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values are 18 and 93 nM for ALK5 binding and for TGF-β cellular assay respectively). inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Orally active.
4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
452342-67-5 C25H23N5O2=425.48
4℃ ≧98%(HPLC) 100 mM in DMSO
515-92431 4242/10 GW 803430 10mg
- 4242/50 50mg
Selective melanin-concentrating hormone receptor 1 (MCH1) antagonist (IC50 = 9.3 nM). Displays antiobesity and antidepressant-like effects in rats and mice. Orally active.
6-(4-Chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one
515141-51-2 C25H24ClN3O3S=481.99
4℃ ≧99%(HPLC) 25 mM in 1eq. HCl
516-68411 2977/1 GW 843682X 1mg
512-68413 2977/10 10mg
- 2977/50 50mg
Selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively). Displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2. inhibits proliferation of most tumor cells in vitro and is selective over normal diploid fibroblasts.
5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide
660868-91-7 C22H18F3N3O4S=477.46
4℃ ≧98%(HPLC) 75 mM in DMSO and to 5 mM in ethanol
519-92831 2649/10 GW 9508 10mg
- 2649/50 50mg
Potent and selective agonist for the free fatty acid receptor FFA1 (GPR40) (pEC50 values are 7.32, < 4.3 and < 4.3 for FFA1, FFA2 and FFA3 receptors respectively). inactive against a range of other GPCRs, kinases, proteases, integrins and PPARs. Potentiates glucose-stimulated insulin secretion in Min6 cells (pEC50 = 6.14).
4-[[(3-Phenoxyphenyl)methyl]amino]benzenepropanoic acid
885101-89-3 C22H21NO3=347.41
RT ≧99%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
516-98701 4650/10 I-BET 151 dihydrochloride 10mg
- 4650/50 50mg
BET bromodomain inhibitor; blocks recruitment of BET to chromatin. induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodent models of MLL-fusion leukemia in vivo. Enhances differentiation of human iPSC into megakaryocytes.
7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride
1883545-47-8 C23H21N5O3.2HCl=488.37
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol and to 100 mM in water
515-69341 1611/10 Lamotrigine 10mg
- 1611/50 50mg
Anticonvulsant. inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Also blocks heterologously expressed and native α4β2 nAChRs with a similar affinity to Na+ channels. Water-soluble salt available (lamotrigine isethionate, Cat. No. 2289).
6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diamine
84057-84-1 C9H7Cl2N5=256.09
RT ≧99%(HPLC) 10 mM in ethanol and to 100 mM in DMSO
- 2289/10 Lamotrigine isethionate 10mg
- 2289/50 50mg
Water-soluble salt of lamotrigine (Cat. No. 1611). Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents.
6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diamine isethionate
113170-86-8 C9H7Cl2N5.C2H6O4S=382.22
RT ≧99%(HPLC) 100 mM in water with gentle warming
517-62081 1264/10 SB 202190 10mg
- 1264/50 50mg
A highly selective, potent and cell-permeable inhibitor of p38 MAP kinase. Binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2 respectively). Promotes stability of naive human pluripotent stem cells in culture. Also available as part of the MAPK inhibitor Tocriset™.
4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol
152121-30-7 C20H14N3OF=331.35
-20℃ ≧99%(HPLC) 100 mM in DMSO
530-50961 0785/10 SB 203186 hydrochloride 10mg
- 0785/50 50mg
Potent 5-HT4 receptor antagonist with high affinity for human atrial 5-HT4 receptors.
1-Piperidinylethyl-1H-indole-3-carboxylate hydrochloride
207572-69-8 C16H20N2O2.HCl=308.81
RT ≧99%(HPLC) 100 mM in water
- 1202/1 SB 203580 1mg
576-71923 1202/10 10mg
570-71921 1202/50 50mg
Selective inhibitor of p38 MAPK (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK-3β and pKBα. Shown to inhibit IL-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase. Enhances clonal growth of skin epithelial progenitor cells; stimulates neural stem cell (NSC) proliferation. Essential component of medium for maintaining stem cells in naive pluripotent state. Part of the MAPK Cascade inhibitor Tocriset™ and MAPK inhibitor Tocriset™. Water-soluble salt SB 203580 hydrochloride (Cat. No. 1402) also available.
4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine
152121-47-6 C21H16FN3OS=377.44
4℃ ≧98%(HPLC) 25 mM in DMSO and to 100 mM in 1eq. HCl
- 1402/10 SB 203580 hydrochloride 10mg
Water-soluble salt of SB 203580 (Cat. No. 1202). Selective inhibitor of p38 mitogen-activated protein kinase (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK3β and pKBα. Shown to inhibit interleukin-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase.
4-[5-(4-Fluorophenyl)-2-[4-(methylsulphonyl)phenyl]-1H-imidazol-4-yl]pyridine hydrochloride
869185-85-3 C21H16FN3OS.HCl=413.89
-20℃ ≧98%(HPLC) 25 mM in water with gentle warming
- 1373/10 SB 204070 10mg
Potent and selective 5-HT4 receptor antagonist (pIC50 = 10.1). Displays >5000-fold selectivity for 5-HT4 over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, and 5-HT3 receptors. Exhibits anxiolytic activity upon systemic administration in vivo.
8-Amino-7-chloro-2,3-dihydro-1,4-benzodioxan-5-carboxylic acid, 1'-butyl-4'-piperidinylmethyl ester
148688-01-1 C19H27ClN2O4.HCl=419.34
RT ≧98%(HPLC) 100 mM in DMSO
552-28531 4962/10 SB 204990 10mg
- 4962/50 50mg
ATP citrate lyase (ACLY) inhibitor. Prodrug of SB 201076. inhibits cholesterol and fatty acid synthesis in a dose-dependent manner in HepG2 cells. Orally active in vivo.
(3R,5S)-rel-5-[6-(2,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid
154566-12-8 C18H22Cl2O5=389.27
-20℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
510-31681 1661/10 SB 206553 hydrochloride 10mg
- 1661/50 50mg
Potent and selective 5-HT2B/5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92). Displays > 80-fold selectivity over all other 5-HT receptor subtypes and a variety of other receptors (pKi < 6). Centrally active following oral administration in vivo.
3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride
1197334-04-5 C17H16N4O.HCl=328.8
RT ≧99%(HPLC) 100 mM in DMSO
- 1374/10 SB 215505 10mg
- 1374/50 50mg
Potent 5-HT2B/2C receptor antagonist (pKi values are 8.3, 7.66 and 6.77 for 5-HT2B, 5-HT2C and 5-HT2A respectively). increases wakefulness and motor activity in rats. Orally active.
6-Chloro-2,3-dihydro-5-methyl-N-5-quinolinyl-1H-indole-1-carboxamide
162100-15-4 C19H16ClN3O=337.81
4℃ ≧98%(HPLC) 100 mM in DMSO
503-37971 1242/10 SB 216641 hydrochloride 10mg
- 1242/50 50mg
A selective h5-HT1B antagonist with approximately 25-fold selectivity over h5-HT1D and little or no affinity for a range of other receptor types.
N-[3-[3-(Dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride
193611-67-5 C28H30N4O4.HCl=523.03
RT ≧98%(HPLC) 50 mM in water
577-72374 1616/1 SB 216763 1mg
573-72371 1616/10 10mg
- 1616/50 50mg
Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 34.3 nM for GSK-3α). Equally effective at inhibiting human GSK-3α and GSK-3β. Exhibits minimal activity against 24 other protein kinases (IC50 >10 μM). Stimulates glycogen synthesis in liver cells, and induces β-catenin-dependent gene transcription. Neuroprotective; also reduces pulmonary inflammation and fibrosis in a mouse model. Shown to maintain mouse embryonic stem cells in a pluripotent state.
3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
280744-09-4 C19H12Cl2N2O2=371.22
RT ≧98%(HPLC) 75 mM in DMSO
- 4672/10 SB 223412 10mg
- 4672/50 50mg
Potent and selective non-peptide NK3 receptor antagonist (Ki values are 1, 144 and >100000 nM for human NK3, NK2 and NK1 receptors respectively). Selective over a panel of >60 receptors, enzymes and ion channels at concentrations of 1 or 10 μM. inhibits NKB-induced Ca2+ mobilization in vitro (IC50 = 16.6 nM) and inhibits NK3-agonist-induced behavioral responses in vivo. Orally active and brain penetrant.
3-Hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide
174636-32-9 C25H22N2O2=382.45
4℃ ≧98%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
556-81791 1221/10 SB 224289 hydrochloride 10mg
- 1221/50 50mg
Selective 5-HT1B receptor antagonist (pKi = 8.2). Displays > 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.
1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine hydrochloride
180084-26-8 C32H32N4O3.HCl=557.09
-20℃ ≧95%(HPLC) 10 mM in DMSO with gentle warming
510-50481 2725/10 SB 225002 10mg
- 2725/50 50mg
Potent and selective CXCR2 chemokine receptor antagonist (IC50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilization in HL60 cells (IC50 values are 8 and 10 nM respectively). Prevents IL-8-induced neutrophil chemotaxis in vitro and sequestration in vivo. inhibits HIV replication in lymphocytes and macrophages.
N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea
182498-32-4 C13H10BrN3O4=352.14
RT ≧99%(HPLC) 100 mM in DMSO and to 50 mM in ethanol
515-96691 1962/10 SB 239063 10mg
Potent and selective p38 MAP kinase inhibitor (IC50 = 44 nM for p38α). Displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580 (Cat. Nos. 1202 and 1402). Reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.
trans-4-[4-(4-Fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]cyclohexanol
193551-21-2 C20H21FN4O2=368.41
4℃ ≧98%(HPLC) 10 mM in DMSO with gentle warming
518-50781 2901/10 SB 242084 10mg
- 2901/50 50mg
5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.
6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride
1215566-78-1 C21H19ClN4O2.2HCl=467.78
4℃ ≧99%(HPLC) 50 mM in DMSO
555-79291 1961/10 SB 258585 hydrochloride 10mg
- 1961/50 50mg
Potent and selective 5-HT6 receptor antagonist (pKi = 8.6); displays > 160-fold selectivity over other 5-HT receptor subtypes.
4-Iodo-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzenesulfonamide hydrochloride
1216468-02-8 C18H22IN3O3S.HCl=523.82
4℃ ≧99%(HPLC) 10 mM in water and to 50 mM in DMSO
517-41581 2726/10 SB 258719 hydrochloride 10mg
- 2726/50 50mg
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
3-Methyl-N-[(1R)-1-methyl-3-(4-methyl-1-piperidinyl)propyl]-N-methylbenzenesulfonamide hydrochloride
1217674-10-6 C18H30N2O2S.HCl=374.97
RT ≧99%(HPLC) 100 mM in water and to 100 mM in DMSO
513-50471 2724/1 SB 265610 1mg
519-50473 2724/10 10mg
- 2724/50 50mg
Potent CXCR2 antagonist that inhibits CinC-1-mediated but not C5a-mediated Ca2+ mobilization (IC50 values are 3.4 and 6800 nM respectively). inhibits CinC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo.
N-(2-Bromophenyl)-N'-(7-cyano-1H-benzotriazol-4-yl)urea
211096-49-0 C14H9BrN6O=357.16
RT ≧98%(HPLC) 100 mM in DMSO and to 10 mM in ethanol
512-92441 4314/10 SB 268262 10mg
- 4314/50 50mg
Selective non-peptide CGRP1 antagonist. inhibits [125I]CGRP binding and CGRP-activated adenylyl cyclase stimulation in SK-N-MC cell membranes (IC50 values are 0.24 and 0.83 nM respectively).
N-Methyl-N-(2-methylphenyl)-3-nitro-4-(2-thiazolylsulfinyl)-benzamide
217438-17-0 C18H15N3O4S2=401.46
RT ≧99%(HPLC) 50 mM in DMSO
558-79301 1612/10 SB 269970 hydrochloride 10mg
- 1612/50 50mg
Potent and selective 5-HT7 receptor antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B and < 6.0 for 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4 and 5-HT6 receptors respectively). Brain penetrant in vivo.
(2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine hydrochloride
261901-57-9 C18H28N2O3S.HCl=388.95
4℃ ≧98%(HPLC) 20 mM in water and to 100 mM in DMSO
519-81841 3368/10 SB 271046 hydrochloride 10mg
- 3368/50 50mg
Selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride
209481-24-3 C20H22ClN3O3S2.HCl=488.45
RT ≧99%(HPLC) 100 mM in DMSO
510-98081 4207/10 SB 277011A dihydrochloride 10mg
- 4207/50 50mg
Selective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and < 5.2 for D3, D2, 5-HT1D and 5-HT1B respectively). Brain penetrant.
N-[trans-4-[2-(6-Cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-4-quinolinecarboxamide dihydrochloride
1226917-67-4 C28H30N4O.2HCl=511.49
4℃ ≧98%(HPLC) 5 mM in water and to 50 mM in DMSO
585-82244 1960/1 SB 334867 1mg
581-82241 1960/10 10mg
587-82243 1960/50 50mg
Selective non-peptide orexin OX1 receptor antagonist. pKB values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.
N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
792173-99-0 C17H13N5O2=319.32
RT ≧99%(HPLC) 100 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
514-23411 1615/10 SB 366791 10mg
- 1615/50 50mg
Potent, selective and competitive vanilloid TRPV1 receptor antagonist (pA2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB1 and CB2 receptors, voltage-gated Ca2+ channels and the hyperpolarization-activated current (Ih). Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.
4'-Chloro-3-methoxycinnamanilide
472981-92-3 C16H14ClNO2=287.75
RT ≧99%(HPLC) 10 mM in ethanol and to 100 mM in DMSO
581-81901 1963/10 SB 408124 10mg
Selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea
288150-92-5 C19H18F2N4O=356.37
RT ≧98%(HPLC) 100 mM in DMSO
580-71461 1617/10 SB 415286 10mg
- 1617/50 50mg
Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 31 nM for GSK-3α); competes with ATP. Has minimal activity against 24 other protein kinases (IC50 > 10 μM). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
3-[(3-Chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
264218-23-7 C16H10ClN3O5=359.73
RT ≧99%(HPLC) 25 mM in ethanol and to 50 mM in DMSO
580-77603 1614/1 SB 431542 1mg
584-77601 1614/10 10mg
Potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF-β-induced proliferation of human osteosarcoma cells. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells. inhibits TGF-β-induced EMT, migration, invasion and VEGF secretion in several human cancer cell lines.
4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
301836-41-9 C22H16N4O3=384.39
RT ≧99%(HPLC) 10 mM in ethanol and to 100 mM in DMSO
514-90343 3265/10 SB 452533 10mg
518-90341 3265/50 50mg
Potent TRPV1 antagonist against capsaicin (pKb = 7.7), noxious heat and acid-mediated (pIC50 = 7.0) receptor activation (pKi = 6.22 at the recombinant hTRPV1 receptor). Exhibits analgesic properties.
N-(2-Bromophenyl)-N'-[2-[ethyl(3-methylphenyl)amino]ethyl]-urea
459429-39-1 C18H22BrN3O=376.29
RT ≧98%(HPLC) 100 mM in DMSO and to 10 mM in ethanol with gentle warming
510-80651 3211/10 SB 525334 10mg
- 3211/50 50mg
Selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells. Attenuates bleomycin-induced pulmonary fibrosis.
6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
356559-20-1 C21H21N5=343.42
-20℃ ≧97%(HPLC) 100 mM in DMSO and 100 mM in 1eq. HCl
515-96451 2650/10 SB 590885 10mg
- 2650/50 50mg
Potent B-Raf inhibitor (Kd = 0.3 nM). Selective for B-Raf against 46 other kinases (Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively). Decreases anchorage-independent growth of melanoma cell lines. inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E.
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
405554-55-4 C27H27N5O2=453.54
-20℃ ≧98%(HPLC) 10 mM in DMSO
554-02731 4670/10 SB 611812 10mg
- 4670/50 50mg
Urotensin-II (UT) antagonist. inhibits urotensin-II-induced proliferation of neonatal cardiac fibroblasts. Attenuates cardiac dysfunction in a rat model of coronary artery ligation; decreases cardiomyocyte hypertrophy, ventricular dilatation and cardiac remodeling.
2,6-Dichloro-N-[4-chloro-3-[2-(dimethylamino)ethoxy]phenyl]-4-(trifluoromethyl)benzenesulfonamide
345892-71-9 C17H16Cl3F3N2O3S=491.74
4℃ ≧99%(HPLC) 10 mM in DMSO
511-92391 3573/10 SB 612111 hydrochloride 10mg
- 3573/50 50mg
Selective NOP receptor antagonist (Ki values are 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively). Antagonizes the pronociceptive action of nociceptin (Cat. No. 0910) in an acute pain model. Potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.
7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride
371980-94-8 C24H29Cl2NO.HCl=454.86
-20℃ ≧97%(HPLC) 100 mM in DMSO and to 100 mM in ethanol
517-92371 3571/10 SB 657510 10mg
- 3571/50 50mg
Selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50 - 189 nM).
2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
474960-44-6 C19H22BrClN2O5S=505.81
RT ≧98%(HPLC) 100 mM in DMSO
- 4673/10 SB 674042 10mg
- 4673/50 50mg
Potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM). Exhibits 100-fold selectivity for OX1 over OX2 receptors. Has no effect at serotonergic, dopaminergic, adrenergic or purinergic receptors. inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.
[5-(2-Fluorophenyl)-2-methyl-4-thiazolyl][2(S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl-1-pyrrolidinyl]methanone
483313-22-0 C24H21FN4O2S=448.51
4℃ 成績書参照 100 mM in DMSO and to 100 mM in ethanol
511-64061 3188/10 SB 699551 10mg
- 3188/50 50mg
Selective 5-HT5A receptor antagonist (pKi values are 8.3, < 6.0, < 6.0, < 6.0, < 5.5 and < 5.5 for 5-HT5A, 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors respectively).
N-[2-(Dimethylamino)ethyl]-N-[[4'-[[(2-phenylethyl)amino]methyl][1,1'-biphenyl]-4-yl]methyl]cyclopentanepropanamide dihydrochloride
864741-95-7 C34H45N3O.2HCl=584.66
4℃ ≧99%(HPLC) 25 mM in DMSO and to 10 mM in ethanol
- 4667/10 SB 706375 10mg
- 4667/50 50mg
High affinity, non-peptide antagonist of the urotensin-II (UT) receptor. Exhibits high affinity for mammalian UT receptors, including human, mouse and rat (Ki values are 9.3, 19.1 and 20.7 nM respectively, in HEK293 cells expressing recombinant UT receptors). Also inhibits binding of radiolabeled urotensin to endogenous human UT receptors (Ki = 5.4 nM in a whole-cell binding assay). Displays greater than or equal to100-fold selectivity for the human UT receptor over 86 different receptors, ion channels, enzymes, transporters and nuclear hormones.
2-Bromo-4,5-dimethoxy-N-[3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]-4-(trifluoromethyl)phenyl]benzenesulfonamide
733734-61-7 C20H22BrF3N2O5S=539.36
RT ≧98%(HPLC) 100 mM in DMSO
- 5040/10 SB 706504 10mg
- 5040/50 50mg
p38 MAPK inhibitor. inhibits LPS-induced transcription of a range of chemokines and cytokines in chronic obstructive pulmonary disease (COPD) monocyte derived macrophages (MDMs). Also inhibits LPS-induced protein expression of IL-6, IL-10, TNFα and γ-inducible protein 10 in COPD MDMs. Effects on suppression of LPS-induced gene and protein expression are enhanced in combination with dexamethasone (Cat. No. 1126).
N-Cyano-N'-[2-[[8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-7,8-dihydro-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]ethyl]guanidine
911110-38-8 C24H19F3N8O=492.46
RT ≧98%(HPLC) 100 mM in DMSO
- 5109/10 SB 743921 hydrochloride 10mg
- 5109/50 50mg
Potent kinesin spindle protein (KSP) inhibitor (Ki = 0.1 nM). induces cell mitotic arrest and apoptosis in vitro. inhibits the growth of a range of tumor cells in vitro, including colon (HCT 116), prostate (PC-3) and leukemia (K-562) cancer cell lines. Causes tumor regression in human tumor xenograft models in vivo, including colon (Colo205), lung (H69) and breast (MCF7) cancer cell xenografts.
N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methylbenzamide hydrochloride
940929-33-9 C31H33ClN2O3.HCl=553.52
-20℃ ≧98%(HPLC) 100 mM in DMSO
550-02711 4630/10 SB 747651A dihydrochloride 10mg
Potent, ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor (IC50 = 11 nM in an in vitro kinase assay); targets the N-terminal kinase domain. inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. Blocks IL-10 production in macrophages.
2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-1H-imidazo[4,5-c]pyridine-7-methanamine dihydrochloride
1781882-72-1 C16H22N8O.2HCl=415.32
RT ≧98%(HPLC) 50 mM in water and to 50 mM in DMSO
510-96521 4118/10 SB 772077B dihydrochloride 10mg
- 4118/50 50mg
Potent Rho-kinase (ROCK) inhibitor (IC50 value of approximately 5.6 nM at recombinant human ROCK1 and 2). Decreases pulmonary and systemic arterial blood pressures and increases cardiac output. Exhibits vasodilator activity that is more potent than Y-27632 (Cat.No 1254) or Fasudil (Cat.No. 0541).
(3S)-1-[[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl]carbonyl]-3-pyrrolidinamine dihydrochloride
607373-46-6 C15H18N8O2.2HCl=415.28
RT ≧99%(HPLC) 100 mM in water and to 100 mM in DMSO
511-29141 1662/10 SKF 77434 hydrobromide 10mg
- 1662/50 50mg
Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.
2,3,4,5-Tetrahydro-1-phenyl-3-(2-propenyl)-1H-3-benzazepine-7,8-diol hydrobromide
300561-58-4 C19H21NO2.HBr=376.29
4℃ ≧99%(HPLC) 10 mM in water and to 100 mM in DMSO
- 1081/10 SKF 89976A hydrochloride 10mg
- 1081/50 50mg
A potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.
1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
85375-15-1 C22H25NO2.HCl=371.91
4℃ ≧99%(HPLC) 100 mM in water with gentle warming and to 100 mM in DMSO
- 1070/10 Zolantidine dimaleate 10mg
- 1070/50 50mg
A potent, selective and brain penetrating H2 receptor antagonist.
N-[3-[3-(1-Piperidinylmethyl)phenoxy]propyl]-2-benzothiazolamine dimaleate
104076-39-3 C22H27N3OS.2C4H4O4=613.68
4℃ - 100 mM in water
 

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