Name: AMG 837 sodium salt
Rating: 5 (10 reviews)

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HIT ID:HIT214314909
Cas No:865231-45-4
常用名:AMG 837 sodium salt
IUPAC:(3S)-3-(4-{[4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]methoxy}phenyl)hex-4-ynoic acid sodium
IUPAC:(3S)-3-(4-{[4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]methoxy}phenyl)hex-4-ynoic acid sodium
InChI key:GLLCPUJEWMFFBZ-BOXHHOBZSA-N

分子式:C26H21F3NaO3
分子量:461.436
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:[Na].CC#C[C@@H](CC(O)=O)c1ccc(OCc2cccc(c2)-c2ccc(cc2)C(F)(F)F)cc1
SMILES:[Na].CC#C[C@@H](CC(O)=O)c1ccc(OCc2cccc(c2)-c2ccc(cc2)C(F)(F)F)cc1

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay.

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