Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.
CAS：1233706-88-1
分子式：C28H25NO6
分子量：471.5
纯度：98%
存储：Store at -20°C

Background:

CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM.IC50 value: 12 nMTarget: cPLA2CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor. It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis. Chinese hamsters (n = 6/group) were infected with parasite-laden contact lenses and treated with cPLA2α inhibitors (AACOCF3 and CAY10650) 50 μg/5 μl was injected with topical eye-drop under the contact lens of an infected cornea three times a day for 6 days and topically on days 7–14 postinfection. Animals were anesthetized and sacrificed 15 days after application of cPLA2α inhibitors. Treatment with the AACOCF3 and CAY10650 had a profound effect on the severity and chronicity of keratitis. In addition, hamsters treated with AACOCF3 had significantly less severe keratitis as compared with CAY10650 group.

参考文献:
[1]. Tripathi T, et al. Role of phospholipase A 2(PLA2) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013 Aug;113:182-91.