CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC 50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Neutrophils Concentration: 12 nM Incubation Time: 30 minutes Result: Inhibited cPLA2-α and inhibited the expression of the p-cPLA2-α. Western Blot AnalysisCell Line: Neutrophils Concentration: 12 nM Incubation Time: 2 hours Result: Inhibited the PGE 2 secretion and inhibited PGE 2 realease.
In Vivo
CAY10650 (50 μg/5 μL; Inject with topical eye-drop; Chinese hamsters) relieves acanthamoeba keratitis in vivo. . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
