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GSK137647A is a diarylsulfonamide that acts as a selective agonist of GPR120 (EC50s = 0.5, 0.63, and 0.79 µM for human, mouse, and rat receptors, respectively).1,2 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.2 It also modestly stimulates the production of glucagon-like peptide-1 in taste bud cells and human intestinal NCI-H716 cells.1,2
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1. Lipid-
2. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg. Med. Chem. Lett. 24, 3100-3103 (2014).