GW9508

First high potency synthetic agonist at GPR40.
GPR40 was formerly an orphan GPCR whose endogenous ligands have been shown to be free fatty acids and has therefore been designated the free fatty acid receptor 1 (FFAR1). It is abundantly expressed on insulin-expressing beta cells and has been shown to mediate the majority of the effects of free fatty acids on insulin secretion. GW9508 enhanced insulin secretion in INS-1E cells and activates ATP-sensitive potassium channels in rat pancreatic beta cells (40μM). It is a useful tool for exploring the biology of GPR40 mediated signaling and physiology.