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 respectively.1 GSK-137647 enhances glucose-stimulated insulin secretion in mouse insulinoma cells and induces intracellular calcium increase in U2OS osteosarcoma cells expressing GPR120.2
4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide is involved in long-chain fatty acid stimulated GLP-1 secretion and has been implicated in glucose homeostasis, adiposity, and regulation of the anti-inflammatory response. It enhances glucose-stimulated insulin secretion in MIN6 cells. It induces intracellular calcium accumulation in U2OS cells; this activity is inhibited by AH 7614.
gsk137647a (50 μm) induced a concentration-dependent increase in glucose (25 mm)-stimulated insulin secretion in min6 mouse insulinoma cell line [1]. in addition, gsk137647a (100 μm) induced a modest increase in glp-1 secretion in the human intestinal cell line nci-h716. moreover, gsk137647a induced intracellular calcium accumulation in u2os cells [1].
gsk137647a (50 μm) induced active glp-1 release by mouse circumvallate papillae (cvps) [2].
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
