| Description | CAY10650 is an effective inhibitor of cytosolic phospholipase A2α (cPLA2α, IC50: 12 nM). |
| In vivo | CAY10650在以0.1 mg/ear剂量局部应用于急性刺激性接触性皮炎的鼠模型中表现出强烈的抗炎效果。在用寄生虫载荷的隐形眼镜感染的中国仓鼠(n=6/组)上,通过将cPLA2α抑制剂(AACOCF3和CAY10650)以50 μg/5 μl剂量以滴眼液的形式注入感染的角膜下隐形眼镜下,每天三次,连续6天,并在感染后7至14天局部应用。实验动物在应用cPLA2α抑制剂15天后被麻醉并牺牲。与CAY10650组相比,AACOCF3和CAY10650的治疗显著降低了角膜炎的严重程度和慢性化,尤其是AACOCF3处理的仓鼠显示出比CAY10650组更轻微的角膜炎症状。 |
| Target activity | CPLA2α:12 nM |
| molecular weight | 471.5 |
| Molecular formula | C28H25NO6 |
| CAS | 1233706-88-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (84.84 mM) |
| References | 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. |