GPR120 (Free Fatty Acid Receptor 4; FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. GSK137647A is a diarylsulfonamide that acts as a selective agonist of GPR120 (pEC50s = 6.3, 6.2, and 6.1 at human, mouse, and rat receptors, respectively). It is selective for GPR120 over a panel of 61 other targets, including other FFARs. Like the natural GPR120 ligand linoleic acid, GSK137647A dose-dependently stimulates insulin secretion by mouse insulinoma MIN6 cells under high glucose conditions. It also modestly stimulates the production of glucagon-like peptide-1 in taste bud cells and human intestinal NCI-H716 cells.
