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Overview
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Background
GPR120 Compound A is an orally active and high-affinity agonist of GPR120 [1].G-protein coupled receptor 120 (GPR120, free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor which has been expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. GPR120 has been involved in mediating the anti-inflammatory and insulin-sensitizing effects of omega 3 fatty acids. Deficiency of GPR120 is responsible for reduced fat metabolism, produce anti-inflammatory effects and to acutely potentiate insulin secretion [2].GPR120 compound A activated GPR120 with the EC50 value of ~0.35 μM. GPR120 compound A demonstrated potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1). In a high-fat diet fed obese mice, GPR120 compound A (30 mg/kg) exerted anti-inflammatory effects on macrophages in vitro and improved glucose tolerance, decreased hyperinsulinemia, increased insulin sensitivity, and decreased hepatic steatosis [1].
[1] Walenta E, Akiyama T E, Lagakos W S, et al. A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice[J]. Nature medicine, 2014, 20(8): 942-947.
[2] Ichimura A, Hirasawa A, Poulain-Godefroy O, et al. Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human[J]. Nature, 2012, 483(7389): 350-354.
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