ATK is an analog of arachidonic acid in which the carboxyl group is replaced by a trifluoromethyl ketone group. It inhibits the activity of the 85 kDa cPLA and the 80 kDa macrophage iPLA without altering the activity of the 14 kDa sPLAs. ATK is useful for differentiating the effects of cPLA and iPLA from sPLA
Arachidonyl Trifluoromethyl Ketone is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. Arachidonyl Trifluoromethyl Ketone is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). Arachidonyl Trifluoromethyl Ketone blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. Arachidonyl Trifluoromethyl Ketone inhibits glucose-induced insulin secretion from isolated rat islets. Arachidonyl Trifluoromethyl Ketone has the potential for the research of cardiovascular disease.
体外研究
Arachidonyl Trifluoromethyl Ketone inhibits the release of arachidonic acid (IC50=8 μM, 2 x 106 cell ml-1) and platelets (IC50=2 μM, 4 x 107 cell ml-1) from U937 cells attacked by calcium ion carriers [1].
Arachidonyl Trifluoromethyl Ketone (10 μM) inhibits phosphate induced calcification and osteogenic/chondrogenic signaling in HAoSMC. Arachidonyl Trifluoromethyl Ketone significantly inhibits basal and Pi induced release of arachidonic acid (a product of PLA2 activity).
体内研究
Arachidonyl Trifluoromethyl Ketone (10 mg/kg; tube feeding method; 5 days a week; ApoE–/- mice (6-week-old male) fed a high cholesterol diet significantly reduced the expression of type III collagen plaques, but had no significant effect on total collagen accumulation.
分子式
C21H31F3O
分子量
356.5
CAS号
149301-79-1
中文名称
花生四烯基三氟甲酮
运输条件
Room temperature in continental US; may vary elsewhere.