AH-7614

AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC₅₀s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC₅₀<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist^[1][2]. IC50 & Target:pIC50: 7.1 (human FFA4)^[1] In Vitro:AH-7614 (compound 39) (0.063-1 μM) blocks intracellular Ca²⁺ response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells^[1].
AH-7614 (100 μM) abolishes the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells^[1].
AH-7614 (0.001-10 μM; 15 min) blocks TUG-891-mediated internalization of FFA4 from the cell surface (pIC₅₀=7.70)^[2].
AH-7614 (10 μM; 30 min) blocks agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4^[2]. In Vivo:AH7614 (50 μg; intratumoral injection once every 4 d for 20 d) reduces the tumor growth in mice^[3].
AH7614 (50 μg; intratumoral injection one day prior to epirubicin injection) enhances cancer cell sensitivity to the chemotherapy and inhibits tumor progression by blocking GPR120 signaling in combination with Epirubicin^[3].