Free fatty acid receptor 4 (FFAR4/GPR120) is a G protein-coupled receptor 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 FFAR4 signaling, resulting in inhibition of toll-like receptor and TNF-α inflammatory signaling pathways in a β-arrestin2/TAB1 dependent manner. AH 7614 is a selective FFAR4 antagonist (pIC50s = 7.1 versus < 4.6 for human FFAR4 and FFAR1 receptors, respectively). In U2OS osteosarcoma cells expressing the FFAR4 receptor, it has been shown to inhibit intracellular calcium accumulation induced by either linoleic acid or an FFAR4 agonist.
