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| Cas No.: | 885101-89-3 |
| Chemical Name: | 3-(4-((3-Phenoxybenzyl)amino)phenyl)propanoic acid |
| Synonyms: | 3-(4-((3-Phenoxybenzyl)amino)phenyl)propanoic acid;4-[[(3-Phenoxyphenyl)methyl]amino]benzenepropanoicacid;GW9508;3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid;GW-9508;4-(3-Phenoxybenzylamino)phenylpropionic acid;GW 9508;Benzenepropanoic acid, 4-[[(3-phenoxyphenyl)methyl]amino]-;3-(4-(3-phenoxybenzylamino)phenyl)propanoic acid;4T77GYP2CS;4-[[(3-Phenoxyphenyl)methyl]amino]benzenepropanoic acid;3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid;Benzenepropanoic acid, 4-(((3-phenoxyphenyl)methyl)amino)-;SMR000486399;3-[4-(3-Phenoxybenzylamino)phenyl]propanoic acid;carboxylic acid agoni |
| SMILES: | O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])N([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])C(=O)O[H] |
| Formula: | C22H21NO3 |
| M.Wt: | 347.407 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.IC50 value: 7.32 (pEC50) [1]Target: GPR40GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. [1] GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. [2] GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes. [3] |