| 產(chǎn)品描述： | CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion |
| 靶點： |
Phospholipase |
| 體外研究： |
CAY10650 (12 nM; 30 min; neutrophils) inhibits the expression of the phosphorylated cPLA2-α (p-cPLA2-α) in cells.CAY10650 (12 nM; 2 h; neutrophils) inhibits PGE2 release in neutrophils. Western Blot Analysis Cell Line: Neutrophils Concentration: 12 nM Incubation Time: 30 minutes Result: Inhibited cPLA2-α and inhibited the expression of the p-cPLA2-α. Western Blot Analysis Cell Line: Neutrophils Concentration: 12 nM Incubation Time: 2 hours Result: Inhibited the PGE2 secretion and inhibited PGE2 realease. |
| 體內(nèi)研究： |
CAY10650 (50 μg/5 μL; Inject with topical eye-drop; Chinese hamsters) relieves acanthamoeba keratitis in vivo.. Animal Model: Chinese hamsters with infected with parasite-laden contact lenses Dosage: 50 μg/5 μL Administration: Inject with topical eye-drop under the contact lens; three times a day for 6 days and topically on days 7 to 20 postinfection Result: Reduced the severity of the keratitis and hasten the onset of resolution.Had little mild inflammation and very few PMNs infiltration in the corneal stroma. |
| 參考文獻： |
1. Paloschi MV, et, al. Cytosolic phospholipase A2-α participates in lipid body formation and PGE2 release in human neutrophils stimulated with an L-amino acid oxidase from Calloselasma rhodostoma venom. Sci Rep. 2020 Jul 3;10(1):10976. 2. Tripathi T, et, al. Role of phospholipase A? (PLA?) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013 Aug;113:182-91. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.121 ml |
10.604 ml |
21.209 ml |
| 5 mM |
0.424 ml |
2.121 ml |
4.242 ml |
| 10 mM |
0.212 ml |
1.06 ml |
2.121 ml |
| 50 mM |
0.042 ml |
0.212 ml |
0.424 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京