AACOCF3

AACOCF3 (Arachidonyl trifluoromethyl ketone) 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^[1][2][3]. In Vitro: AACOCF3 inhibits the release of arachidonic acid from calcium ionophore-challenged U937 cells (IC₅₀= 8 μM, 2 x 10⁶ cells ml^-1) and from platelets (IC₅₀= 2 μM, 4 x 10⁷ cells ml^-1)^[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]. In Vivo: 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].