4-[2-(2-methylphenyl)ethynyl]-benzenepropanoicacid

Biological Activity

TUG-424 is expected to be useful in the exploration of FFA1 and may also be valuable as a lead structure for new potential antidiabetic therapeutics. TUG-424 significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity. It enhanced glucose-stimulated insulin secretion in a r at beta-cell line already at 100 nM and from isolated mouse islets through FFA1.

GPR40 (now FFA1) was formerly an orphan GPCR whose endogenous ligands have recently been identified as free fatty acids (FFAs). The receptor appears to be involved in the pathophysiology of type 2 diabetes and is a drug target because of its role in FFA-mediated enhancement of glucose-stimulated insulin release.