GPR120 (free fatty acid receptor 4; FFAR4) is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. ω-3 Fatty acids, such as docosahexaenoic acid and eicosapentaenoic acid , initiate GPR120 signaling resulting in inhibition of toll-like receptor and TNF-α inflammatory signaling pathways in a β-arrestin2/TAB1 dependent manner. TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively. It activates GPR40 (FFAR1) with a pEC50 value of 4.19 and shows no activity at GPR41 (FFAR3) or GPR43 (FFAR2).
