Free Fatty Acid Receptor (FFAR)

TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.

GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.

GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors.

AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.

GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.

TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.

DC260126, a small-molecule antagonist of GPR40.