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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。

 

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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
-5256/10AH 761410mg
-5256/5050mg
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
6326-06-3C20H17NO3S=351.42
4℃≧98%(HPLC)100 mM in DMSO
550-792411207/10BRL 15572 hydrochloride10mg
-1207/5050mg
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
1173022-77-9C25H27ClN2O.HCl=443.42
4℃-10 mM in DMSO and to 50 mM in ethanol
522-449910948/10BRL 37344, sodium salt10mg
528-449930948/5050mg
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
127299-93-8C19H21NO4ClNa=385.82
RT≧98%(HPLC)100 mM in water
501-383711133/10BRL 44408 maleate10mg
-1133/5050mg
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
681806-46-2C13H17N3.C4H4O4=331.37
-20℃≧98%(HPLC)100 mM in water
-2237/10BRL 5048110mg
-2237/5050mg
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
433695-36-4C9H12N2O4S=244.26
4℃≧99%(HPLC)100 mM in ethanol and to 100 mM in DMSO
-0699/10BRL 52537 hydrochloride10mg
-0699/5050mg
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
112282-24-3C18H24Cl2N2O.HCl=391.77
RT≧98%(HPLC)5 mM in water with gentle warming
-1663/10BW 373U8610mg
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
155836-50-3C27H37N3O2=435.61
4℃≧99%(HPLC)100 mM in 1eq. HCl
551-027414674/10CZC 2483210mg
-4674/5050mg
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
1159824-67-5C15H17FN6O2S=364.4
4℃≧98%(HPLC)100 mM in DMSO
516-806312902/10D 447610mg
-2902/5050mg
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
301836-43-1C23H18N4O3=398.41
4℃≧99%(HPLC)100 mM in DMSO and to 50 mM in ethanol
557-027214646/10Elacridar hydrochloride10mg
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
143851-98-3C34H33N3O5.HCl=600.1
-20℃≧99%(HPLC)20 mM in DMSO
514-291311659/10Fenoldopam hydrochloride10mg
-1659/5050mg
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
181217-39-0C16H16ClNO3.HCl=342.22
4℃≧98%(HPLC)10 mM in water
554-758612007/10Fluticasone propionate10mg
-2007/5050mg
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
80474-14-2C25H31F3O5S=500.57
RT≧98%(HPLC)50 mM in DMSO
510-923612348/10Gavestinel10mg
-2348/5050mg
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
153436-38-5C18H11Cl2N2O3Na=397.19
RT≧98%(HPLC)40 mM in DMSO
-3995/1GI 254023X1mg
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
260264-93-5C21H33N3O4=391.5
-20℃≧98%(HPLC)20 mM in DMSO
577-717911322/10GR 11380810mg
-1322/5050mg
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
144625-51-4C19H27N3O4S=393.5
RT≧98%(HPLC)25 mM in 1eq. HCl
513-316711658/10GR 125487 sulfamate10mg
-1658/5050mg
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
859502-43-5C19H26FN3O5S.H2NSO3H=524.58
RT≧97%(HPLC)10 mM in water with gentle warming
516-326411274/10GR 15989710mg
-1274/5050mg
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
158848-32-9C23H27FN2O2S=414.54
-20℃≧97%(HPLC)50 mM in DMSO and to 10 mM in ethanol
539-509310864/10GR 4661110mg
-0864/5050mg
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
185259-85-2C23H27N3O2=377.49
RT-50 mM in DMSO and to 10 mM in ethanol
573-987511054/10GR 55562 dihydrochloride10mg
-1054/5050mg
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
159533-25-2C23H25N3O2.2HCl=448.39
4℃≧98%(HPLC)100 mM in water
-1668/1GR 643491mg
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.
-
137593-52-3C42H68N10O11S=921.12
-20℃成績書参照1 mg/ml in water
-1669/1GR 736321mg
Potent and selective tachykinin NK1 receptor agonist (EC50 = 2 nM in guinea pig vas deferens). Active in vivo.
-
133156-06-6C40H59N7O6S=766.01
-20℃成績書参照1 mg/ml in water
-1957/10GR 7923610mg
-1957/5050mg
Adenosine A1 receptor agonist (Ki = 3.1 nM). Anticonvulsive in mice following systemic administration in vivo.
N-[(1S,2S)-2-Hydroxycyclopentyl]adenosine
124555-18-6C15H21N5O5=351.36
4℃≧99%(HPLC)100 mM in water
-1670/1GR 823341mg
Tachykinin NK1 receptor antagonist.
-
129623-01-4C69H91N15O16=1386.57
-20℃成績書参照1 mg/ml in water
-1667/1GR 948001mg
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.
-
141636-65-9C49H61N9O8=904.08
-20℃成績書参照4 mg/ml in ethanol
511-924114026/10GSK 105961510mg
-4026/5050mg
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
958852-01-2C18H11N3O2S=333.36
4℃≧98%(HPLC)10 mM in DMSO
-5110/10GSK 1562590 hydrochloride10mg
-5110/5050mg
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
1003878-07-6C30H30Cl2N4O4.HCl=617.95
4℃≧98%(HPLC)100 mM in DMSO
-5111/10GSK 183870510mg
-5111/5050mg
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
1116235-97-2C27H29FN8O3=532.57
-20℃≧98%(HPLC)100 mM in DMSO
558-293515257/10GSK 13764710mg
-5257/5050mg
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
349085-82-1C16H19NO3S=305.39
RT≧99%(HPLC)100 mM in DMSO and to 50 mM in ethanol
-5106/5GSK 21938745mg
-5106/2525mg
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
1336960-13-4C37H38BrF3N4O=691.62
4℃≧98%(HPLC)20 mM in 1eq. HCl and to 50 mM in DMSO
-5303/5GSK 21940695mg
-5303/2525mg
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
1332331-08-4C25H24N4O3=428.48
4℃≧99%(HPLC)100 mM in DMSO and to 20 mM in ethanol
517-965314143/10GSK 233447010mg
513-965334143/5050mg
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
1227911-45-6C25H34N8O=462.59
4℃≧98%(HPLC)100 mM in DMSO and to 100 mM in ethanol
-4629/5GSK 2578215A5mg
-4629/2525mg
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
1285515-21-0C24H18FN3O2=399.42
RT≧99%(HPLC)100 mM in DMSO
-5107/10GSK 260641410mg
-5107/5050mg
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
1337531-36-8C24H20F3N50=451.44
-20℃≧99%(HPLC)100 mM in DMSO
513-965114009/10GSK 26996210mg
-4009/5050mg
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
850664-21-0C29H30N8O5=570.6
4℃≧99%(HPLC)100 mM in DMSO and to 10 mM in ethanol with gentle warming
-5140/10GSK 283037110mg
-5140/5050mg
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
1404456-53-6C23H29ClN4O2S=461.02
-20℃≧98%(HPLC)100 mM in DMSO and to 50 mM in ethanol
550-315215189/10GSK 2837808A10mg
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
1445879-21-9C31H25F2N5O7S=649.62
-20℃≧98%(HPLC)100 mM in DMSO
514-924013726/1GSK 4292861mg
-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
864082-47-3C21H16F4N4O2=432.37
4℃≧97%(HPLC)100 mM in DMSO and to 25 mM in ethanol
514-923813572/10GSK 65039410mg
-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
890842-28-1C25H22N2O2=382.45
RT≧97%(HPLC)100 mM in DMSO
511-903534144/10GSK 69069310mg
515-903514144/5050mg
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
937174-76-0C21H27N7O3=425.48
-20℃≧98%(HPLC)50 mM in DMSO
518-924214116/10GSK 902710mg
-4116/5050mg
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
1229096-88-1C27H19F4N3O2S=525.52
RT≧98%(HPLC)100 mM in DMSO
514-004512229/10GW 074210mg
-2229/5050mg
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
317318-84-6C21H17F4NO3S2=471.49
4℃≧98%(HPLC)50 mM in ethanol and to 100 mM in DMSO
511-004611664/10GW 1929 hydrochloride10mg
-1664/5050mg
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
1217466-21-1C30H29N3O4.HCl=532.03
4℃≧98%(HPLC)100 mM in ethanol with gentle warming and to 100 mM in water
518-964412474/1GW 3965 hydrochloride1mg
-2474/1010mg
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
405911-17-3C33H31NO3ClF3.HCl=618.51
RT≧98%(HPLC)100 mM in DMSO and to 20 mM in ethanol
511-326912473/10GW 406410mg
-2473/5050mg
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
278779-30-9C28H22Cl3NO4=542.84
4℃≧97%(HPLC)100 mM in DMSO and to 10 mM in ethanol
-2238/10GW 44175610mg
-2238/5050mg
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
504433-23-2C17H13N3O=275.31
RT≧99%(HPLC)15 mM in DMSO
-1381/10GW 507410mg
-1381/5050mg
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
512-207712239/10GW 583340 dihydrochloride10mg
-2239/5050mg
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
1173023-85-2C28H25ClFN5O3S2.2HCl=671.03
4℃≧97%(HPLC)100 mM in DMSO with gentle warming
-4668/10GW 62736810mg
-4668/5050mg
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
439288-66-1C30H28N2O6S=544.62
-20℃≧98%(HPLC)100 mM in DMSO
513-967514618/10GW 647110mg
-4618/5050mg
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
880635-03-0C35H36F3N3O4=619.67
4℃≧98%(HPLC)75 mM in DMSO and to 20 mM in ethanol
515-004811677/10GW 764710mg
-1677/5050mg
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
265129-71-3C29H46N2O3S=502.75
RT≧99%(HPLC)25 mM in ethanol and to 100 mM in DMSO
519-964713264/10GW 78838810mg
-3264/5050mg
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
452342-67-5C25H23N5O2=425.48
4℃≧98%(HPLC)100 mM in DMSO
515-924314242/10GW 80343010mg
-4242/5050mg
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
515141-51-2C25H24ClN3O3S=481.99
4℃≧99%(HPLC)25 mM in 1eq. HCl
516-684112977/1GW 843682X1mg
512-684132977/10 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
660868-91-7C22H18F3N3O4S=477.46
4℃≧98%(HPLC)75 mM in DMSO and to 5 mM in ethanol
519-928312649/10GW 950810mg
-2649/5050mg
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
885101-89-3C22H21NO3=347.41
RT≧99%(HPLC)100 mM in DMSO and to 100 mM in ethanol
516-987014650/10I-BET 151 dihydrochloride10mg
-4650/5050mg
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
1883545-47-8C23H21N5O3.2HCl=488.37
-20℃≧98%(HPLC)100 mM in DMSO and to 100 mM in ethanol and to 100 mM in water
515-693411611/10Lamotrigine10mg
-1611/5050mg
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
84057-84-1C9H7Cl2N5=256.09
RT≧99%(HPLC)10 mM in ethanol and to 100 mM in DMSO
-2289/10Lamotrigine isethionate10mg
-2289/5050mg
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
113170-86-8C9H7Cl2N5.C2H6O4S=382.22
RT≧99%(HPLC)100 mM in water with gentle warming
517-620811264/10SB 20219010mg
-1264/5050mg
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
152121-30-7C20H14N3OF=331.35
-20℃≧99%(HPLC)100 mM in DMSO
530-509610785/10SB 203186 hydrochloride10mg
-0785/5050mg
Potent 5-HT4 receptor antagonist with high affinity for human atrial 5-HT4 receptors.
1-Piperidinylethyl-1H-indole-3-carboxylate hydrochloride
207572-69-8C16H20N2O2.HCl=308.81
RT≧99%(HPLC)100 mM in water
-1202/1SB 2035801mg
576-719231202/10 10mg
570-719211202/50 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
152121-47-6C21H16FN3OS=377.44
4℃≧98%(HPLC)25 mM in DMSO and to 100 mM in 1eq. HCl
-1402/10SB 203580 hydrochloride10mg
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
869185-85-3C21H16FN3OS.HCl=413.89
-20℃≧98%(HPLC)25 mM in water with gentle warming
-1373/10SB 20407010mg
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
148688-01-1C19H27ClN2O4.HCl=419.34
RT≧98%(HPLC)100 mM in DMSO
552-285314962/10SB 20499010mg
-4962/5050mg
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
154566-12-8C18H22Cl2O5=389.27
-20℃≧98%(HPLC)100 mM in DMSO and to 100 mM in ethanol
510-316811661/10SB 206553 hydrochloride10mg
-1661/5050mg
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
1197334-04-5C17H16N4O.HCl=328.8
RT≧99%(HPLC)100 mM in DMSO
-1374/10SB 21550510mg
-1374/5050mg
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
162100-15-4C19H16ClN3O=337.81
4℃≧98%(HPLC)100 mM in DMSO
503-379711242/10SB 216641 hydrochloride10mg
-1242/5050mg
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
193611-67-5C28H30N4O4.HCl=523.03
RT≧98%(HPLC)50 mM in water
577-723741616/1SB 2167631mg
573-723711616/10 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
280744-09-4C19H12Cl2N2O2=371.22
RT≧98%(HPLC)75 mM in DMSO
-4672/10SB 22341210mg
-4672/5050mg
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
174636-32-9C25H22N2O2=382.45
4℃≧98%(HPLC)100 mM in DMSO and to 100 mM in ethanol
556-817911221/10SB 224289 hydrochloride10mg
-1221/5050mg
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
180084-26-8C32H32N4O3.HCl=557.09
-20℃≧95%(HPLC)10 mM in DMSO with gentle warming
510-504812725/10SB 22500210mg
-2725/5050mg
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
182498-32-4C13H10BrN3O4=352.14
RT≧99%(HPLC)100 mM in DMSO and to 50 mM in ethanol
515-966911962/10SB 23906310mg
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
193551-21-2C20H21FN4O2=368.41
4℃≧98%(HPLC)10 mM in DMSO with gentle warming
518-507812901/10SB 24208410mg
-2901/5050mg
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
1215566-78-1C21H19ClN4O2.2HCl=467.78
4℃≧99%(HPLC)50 mM in DMSO
555-792911961/10SB 258585 hydrochloride10mg
-1961/5050mg
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
1216468-02-8C18H22IN3O3S.HCl=523.82
4℃≧99%(HPLC)10 mM in water and to 50 mM in DMSO
517-415812726/10SB 258719 hydrochloride10mg
-2726/5050mg
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
1217674-10-6C18H30N2O2S.HCl=374.97
RT≧99%(HPLC)100 mM in water and to 100 mM in DMSO
513-504712724/1SB 2656101mg
519-504732724/10 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
211096-49-0C14H9BrN6O=357.16
RT≧98%(HPLC)100 mM in DMSO and to 10 mM in ethanol
512-924414314/10SB 26826210mg
-4314/5050mg
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
217438-17-0C18H15N3O4S2=401.46
RT≧99%(HPLC)50 mM in DMSO
558-793011612/10SB 269970 hydrochloride10mg
-1612/5050mg
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
261901-57-9C18H28N2O3S.HCl=388.95
4℃≧98%(HPLC)20 mM in water and to 100 mM in DMSO
519-818413368/10SB 271046 hydrochloride10mg
-3368/5050mg
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
209481-24-3C20H22ClN3O3S2.HCl=488.45
RT≧99%(HPLC)100 mM in DMSO
510-980814207/10SB 277011A dihydrochloride10mg
-4207/5050mg
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
1226917-67-4C28H30N4O.2HCl=511.49
4℃≧98%(HPLC)5 mM in water and to 50 mM in DMSO
585-822441960/1SB 3348671mg
581-822411960/10 10mg
587-822431960/50 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
792173-99-0C17H13N5O2=319.32
RT≧99%(HPLC)100 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
514-234111615/10SB 36679110mg
-1615/5050mg
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
472981-92-3C16H14ClNO2=287.75
RT≧99%(HPLC)10 mM in ethanol and to 100 mM in DMSO
581-819011963/10SB 40812410mg
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
288150-92-5C19H18F2N4O=356.37
RT≧98%(HPLC)100 mM in DMSO
580-714611617/10SB 41528610mg
-1617/5050mg
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
264218-23-7C16H10ClN3O5=359.73
RT≧99%(HPLC)25 mM in ethanol and to 50 mM in DMSO
580-776031614/1SB 4315421mg
584-776011614/1010mg
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
301836-41-9C22H16N4O3=384.39
RT≧99%(HPLC)10 mM in ethanol and to 100 mM in DMSO
514-903433265/10SB 45253310mg
518-903413265/5050mg
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
459429-39-1C18H22BrN3O=376.29
RT≧98%(HPLC)100 mM in DMSO and to 10 mM in ethanol with gentle warming
510-806513211/10SB 52533410mg
-3211/5050mg
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
356559-20-1C21H21N5=343.42
-20℃≧97%(HPLC)100 mM in DMSO and 100 mM in 1eq. HCl
515-964512650/10SB 59088510mg
-2650/5050mg
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
405554-55-4C27H27N5O2=453.54
-20℃≧98%(HPLC)10 mM in DMSO
554-027314670/10SB 61181210mg
-4670/5050mg
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
345892-71-9C17H16Cl3F3N2O3S=491.74
4℃≧99%(HPLC)10 mM in DMSO
511-923913573/10SB 612111 hydrochloride10mg
-3573/5050mg
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
371980-94-8C24H29Cl2NO.HCl=454.86
-20℃≧97%(HPLC)100 mM in DMSO and to 100 mM in ethanol
517-923713571/10SB 65751010mg
-3571/5050mg
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
474960-44-6C19H22BrClN2O5S=505.81
RT≧98%(HPLC)100 mM in DMSO
-4673/10SB 67404210mg
-4673/5050mg
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
483313-22-0C24H21FN4O2S=448.51
4℃成績書参照100 mM in DMSO and to 100 mM in ethanol
511-640613188/10SB 69955110mg
-3188/5050mg
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
864741-95-7C34H45N3O.2HCl=584.66
4℃≧99%(HPLC)25 mM in DMSO and to 10 mM in ethanol
-4667/10SB 70637510mg
-4667/5050mg
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
733734-61-7C20H22BrF3N2O5S=539.36
RT≧98%(HPLC)100 mM in DMSO
-5040/10SB 70650410mg
-5040/5050mg
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
911110-38-8C24H19F3N8O=492.46
RT≧98%(HPLC)100 mM in DMSO
-5109/10SB 743921 hydrochloride10mg
-5109/5050mg
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
940929-33-9C31H33ClN2O3.HCl=553.52
-20℃≧98%(HPLC)100 mM in DMSO
550-027114630/10SB 747651A dihydrochloride10mg
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
1781882-72-1C16H22N8O.2HCl=415.32
RT≧98%(HPLC)50 mM in water and to 50 mM in DMSO
510-965214118/10SB 772077B dihydrochloride10mg
-4118/5050mg
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
607373-46-6C15H18N8O2.2HCl=415.28
RT≧99%(HPLC)100 mM in water and to 100 mM in DMSO
511-291411662/10SKF 77434 hydrobromide10mg
-1662/5050mg
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
300561-58-4C19H21NO2.HBr=376.29
4℃≧99%(HPLC)10 mM in water and to 100 mM in DMSO
-1081/10SKF 89976A hydrochloride10mg
-1081/5050mg
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
85375-15-1C22H25NO2.HCl=371.91
4℃≧99%(HPLC)100 mM in water with gentle warming and to 100 mM in DMSO
-1070/10Zolantidine dimaleate10mg
-1070/5050mg
A potent, selective and brain penetrating H2 receptor antagonist.
N-[3-[3-(1-Piperidinylmethyl)phenoxy]propyl]-2-benzothiazolamine dimaleate
104076-39-3C22H27N3OS.2C4H4O4=613.68
4℃-100 mM in water
 

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