AH 7614

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.^1,2 ω-3 Fatty acids, such as docosahexaenoic acid (Item No. 90310) and eicosapentaenoic acid (Item No. 90110), initiate FFAR4 signaling, resulting in inhibition of toll-like receptor and TNF-α inflammatory signaling pathways in a β-arrestin2/TAB1 dependent manner.² AH 7614 is a selective FFAR4 antagonist (IC₅₀s = 0.079 and 25 µM for human FFAR4 and FFAR1 receptors, respectively).³ 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.³

WARNING This product is not for human or veterinary use.

1. Davenport, A.P., Alexander, S.P.H., Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacol. Rev. 65(3), 967-986 (2013).

2. Oh, D.Y., Talukdar, S., Bae, E.J., et al. GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin sensitizing effects. Cell 142(5), 687-698 (2010).

3. Sparks, S.M., Chen, G., Collins, J.L., et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA₄/GPR120). Bioorg. Med. Chem. Lett. 24, 3100-3103 (2014).