产品
编 号:F574174
分子式:C20H17NO3S
分子量:351.42
产品类型
结构图
CAS No: 6326-06-3
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产品详情
生物活性:
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.
体内研究:
AH7614 (50 μg; intratumoral injection once every 4 d for 20 d) reduces the tumor growth in mice.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.
体外研究:
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.AH-7614 (100 μM) abolishes the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells.AH-7614 (0.001-10 μM; 15 min) blocks TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70).AH-7614 (10 μM; 30 min) blocks agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4.