Biological Activity
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].
References
[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.
