AACOCF3 是花生四烯酸的可渗透细胞的三氟甲基酮类似物。AACOCF3 是 85-kDa 胞质磷脂酶 A2 (cPLA2) 的有效选择性慢结合抑制剂。AACOCF3 阻止钙离子载体攻击的血小板产生花生四烯酸和 12-羟基二十碳四烯酸。 AACOCF3 抑制离体大鼠胰岛葡萄糖诱导的胰岛素分泌。AACOCF3 具有研究心脑血管疾病的潜力。

AACOCF3 is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.

AACOCF3 inhibits the release of arachidonic acid from calcium ionophore-challenged U937 cells with IC50 of 8 μM and from platelets with IC50 of 2 μM[1]. AACOCF3 (10 μM) suppresses phosphate-induced calcification and osteogenic/chondrogenic signaling in HAoSMCs. AACOCF3 significantly inhibits both basal and Pi-induced release of arachidonic acid, the product of PLA2 activity[2].

AACOCF3 (10 mg/kg; gavage; 5 days a week; ApoE–/– mice (6-week-old males) were fed a high-cholesterol diet) significantly reduces type III collagen plaque expression, but had no significant influence on total collagen accumulation[3].

149301-79-1

C21H31F3O

356.47

Arachidonyl trifluoromethyl ketone;Arachidonyltrifluoromethane

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years