AMG 837 calcium hydrate 是口服有效的GPR40/FFA1部分激动剂，抑制 [3H]AMG 837 与人类FFA1受体的特异性结合，pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。

AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 >10,000 nM).

GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50: 13 nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50s: 23/13 nM). AMG 837 was a partial agonist on GPR40 with maximal activity 85% of that shown by DHA. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50: 3 μM) on the α2-adrenergic receptor [1].

In rats, AMG 837 increases insulin release when glucose levels are elevated [2].

1259389-38-2

C26H23F3O4·1/2Ca

476.5

DMSO:40 mg/mL (87.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years