AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 holds promise for cardiovascular disease research.

AACOCF3以IC50 8 μM抑制钙离子载体挑战的U937细胞中的花生四烯酸释放，以及以IC50 2 μM抑制血小板中的释放[1]。AACOCF3 (10 μM)可显著抑制磷酸盐诱导的钙化和HAoSMCs中的成骨/成软骨信号传导。AACOCF3有效抑制PLA2活性产物——花生四烯酸的基础及Pi诱导的释放[2]。

AACOCF3（10 mg/kg；灌胃；每周5天；6周龄雄性ApoE–/–小鼠，喂食高胆固醇饮食）显著降低了III型胶原斑块表达，但对总胶原蛋白积累无显著影响[3]。