FFA4 (GPR120) is a potential 7TM receptor involved in long-chain fatty acid-stimulated secretion of antidiabetic hormone glucagon-like peptide-1 (GLP1). GSK137647A is a selective FFA4 agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse, and rat FFA4, respectively. GSK137647A dose-dependently increased high glucose (25mM)-stimulated insulin secretion from MIN6 mouse insulinoma cells. Treatment of human intestinal cell line NCI-H716 with GSK137647A (100μM) resulted in a modest increase in GLP-1 secretion[2]. Incubation with 50μM GSK137647A induced the release of active GLP-1 by freshly isolated mouse circumvallate papillae[3]. Supplementation with GSK137647A (20mg/kg) every 2 days for 4 weeks ameliorated fat diet-induced glucose intolerance and insulin insensitivity in WT mice but not GPR120 knockout mice[4].
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