AM-3189

AM-3189 is an orally active and selective GPR40 agonist with EC50 values in buffer solution and in 100% human serum of 33 nM and 10 μM respectively. AM-3189 shows no significant activity on GPR41 and GPR43, and no agonistic activity on PPAR-α, -δ, and -γ. AM-3189 enhances glucose-stimulated insulin secretion by activating GPR40 on pancreatic β cells. AM-3189 has extremely low penetration into the central nervous system and significantly reduces blood glucose levels in two humanized GPR40 mouse models. AM-3189 can be used for the study of type 2 diabetes[1].