GSK137647A

GSK137647A is a a selective agonist of FFA4 (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.