CAY10650 是高效的胞浆磷脂酶A2α抑制剂,IC50=12 nM,能够抑制脂滴形成和 PGE2 分泌。
产品描述
CAY10650 is an effective inhibitor of cytosolic phospholipase A2α (cPLA2α, IC50: 12 nM).
体内活性
CAY10650 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 the 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 the CAY10650 group.
Cas No.
1233706-88-1
分子式
C28H25NO6
分子量
471.5
储存和溶解度
DMSO:40 mg/mL (84.84 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years