AH-7614 demonstrates potent and selective antagonism against FFA4 (GPR120), with pIC50 values of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. It exhibits selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 effectively inhibits the actions of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist[1].[2].
体内研究
AH7614 (50 μg; intratumoral injection once every 4 days for 20 days) decreases tumor growth in mice[3].
AH7614 (50 μg; intratumoral injection one day prior to epirubicin injection) enhances cancer cell sensitivity to chemotherapy and inhibits tumor progression by blocking GPR120 signaling in combination with Epirubicin[3].
体外研究
AH-7614 (0.063-1 μM) inhibits the intracellular Ca2+ response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells[1].
AH-7614 (100 μM) eliminates the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells[1].
AH-7614 (0.001-10 μM; 15 min) prevents TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70)[2].
AH-7614 (10 μM; 30 min) inhibits agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4[2].
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