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AMG 837
CAS No. : 865231-46-5
Biological Activity:AMG 837 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 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. 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. showed
no significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potent
and selective in vitro.
Research Area:Metabolic Disease
Targets:Free Fatty Acid Receptor
Related Small Molecules:GW-1100;Grifolic acid;Ginsenoside Rb2;AP5;GPR40 Activator 1;AM-1638;DC260126;TUG-770;LY2881835;FFA1 agonist-1;GPR120 Agonist 3;AS2034178 free base;GPR40 Agonist 2;BMS-986118;AMG7703;Fasiglifam;MEDICA16;AR420626;AMG 837 sodium salt;Xelaglifam;TUG-1375;GPR120 Agonist 1;GPR40 agonist 5;TUG-424;GPR120 modulator 2;LY2922470;4-CMTB
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