amg 837

AMG 837 is a potent and orally bioavailable small molecule partial agonist of the GPR40 receptor (also known as free fatty acid receptor 1 or FFA1). It stimulates calcium flux in cells expressing human GPR40 with an EC50 of approximately 13.5 nM. In preclinical studies, AMG 837 enhanced glucose-stimulated insulin secretion both in vitro and in vivo and lowered postprandial glucose levels during glucose tolerance tests in normal and Zucker fatty rats. The improvement in glucose excursions persisted following daily dosing for up to 21 days. These findings support its potential utility for the treatment of type 2 diabetes[1][5][7]. However, while it showed promise preclinically by lowering blood glucose and increasing insulin secretion in animal models, it did not significantly increase insulin release or improve glucose levels in healthy volunteers during Phase I clinical trials[8][9]. Additionally, recent research has identified that AMG 837 calcium hydrate can act as a potent inhibitor of Brucella by targeting BacA protein[4].

Other names

865231-46-5UNII-NE6U6R66U4UNII-NE-6U6R66U4UNII-NE 6U6R66U4NE6U6R66U4NE-6U6R66U4NE 6U6R66U4(3S)-3-[4-({3-[4-(trifluoromethyl)phenyl]phenyl}methoxy)phenyl]hex-4-ynoic acid