GSK-137647 (349085-82-1) is a potent and selective agonist at free fatty acid receptor 4 (FFA4), also known as GPR120. pEC50s= 6.3, 6.2 and 6.1 for human, mouse and rat receptor respectively1. GSK-137647 enhances glucose-stimulated insulin secretion in mouse insulinoma cells and induces intracellular calcium increase in U2OS osteosarcoma cells expressing GPR1202.
1) Martin et al. (2012), Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity; J. Lipid Res., 53 2256
2) Sparks et al. (2014), Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120); Bioorg. Med. Chem. Lett., 24 3100