AACOCF3  (Synonyms: Arachidonyl trifluoromethyl ketone)

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].

AACOCF3 抑制钙离子载体攻击的 U937 细胞释放花生四烯酸 (IC₅₀= 8 μM，2 x 10⁶ 细胞 ml^-1) 和血小板 (IC₅₀= 2 μM，4 x 10⁷ 细胞 ml^-1)^[1]。
AACOCF3 (10 μM) 抑制 HAoSMC 中磷酸盐诱导的钙化和成骨/软骨形成信号。AACOCF3 显著抑制基础和 Pi 诱导的花生四烯酸 (PLA2 活性的产物) 释放^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AACOCF3 (10 mg/kg；管饲法；每周 5 天；ApoE^–/– 小鼠 (6 周龄雄性) 喂食高胆固醇饮食) 显著减少 III 型胶原蛋白斑块表达，但对总胶原蛋白积累没有显著影响^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

356.47

C₂₁H₃₁F₃O

149301-79-1

液体

Colorless to light yellow

Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years

• [1]. Riendeau D, et al. Arachidonyl trifluoromethyl ketone, a potent inhibitor of 85-kDa phospholipase A2, blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. J Biol Chem. 1994;269(22):15619-15624.  [Content Brief]

  [2]. Schanstra JP, et al. Systems biology identifies cytosolic PLA2 as a target in vascular calcification treatment. JCI Insight. 2019;4(10):e125638. Published 2019 May 16.  [Content Brief]

  [3]. Loweth AC, et al. A specific inhibitor of cytosolic phospholipase A2 activity, AACOCF3, inhibits glucose-induced insulin secretion from isolated rat islets. Biochem Biophys Res Commun. 1996;218(2):423-427.  [Content Brief]