Favorite  |  Set Home
Products > Others > > CAY10650
Product name : CAY10650
Item : CR1776
Price : 200mg, $950;500mg, $1695; 1g, $2490; 2g, $3590
contact : Send inquiry to: info@acesobio.com
CAS : 1233706-88-1
Molecular Weight : 471.5
Formula : C₂₈H₂₅NO₆
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
 Enlarge Image                   Back
←[Previous Product]              [Next Product]→


Details:
 Chemical Information
M.Wt 471.5 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C28H25NO6
CAS No 1233706-88-1
Solubility

DMSO



Biological Activity of CAY10650

 

CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) in hibitor with an IC50 value of 12 nM.
IC50 value: 12 nM
Target: cPLA2
CAY10650 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.

 

[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.
Abstract
The aim of this study is to determine if the mannose-induced protein (MIP-133) from Acanthamoeba castellanii trophozoites induces apoptosis of corneal epithelial cells through a cytosolic phospholipase A2α (cPLA2α)-mediated pathway. The efficacy of cPLA2α inhibitors to provide protection against Acanthamoeba keratitis was examined in vivo. Chinese hamster corneal epithelial (HCORN) cells were incubated with or without MIP-133. MIP-133 induces significant increase in cPLA2α and macrophage inflammatory protein-2 (MIP-2/CXCL2) levels from corneal cells. Moreover, cPLA2α inhibitors, MAFP (Methyl-arachidonyl fluorophosphonate) and AACOCF3 (Arachidonyl trifluoromethyl ketone), significantly reduce cPLA2α and CXCL2 from these cells (P < 0.05). Additionally, cPLA2α inhibitors significantly inhibit MIP-133-induced apoptosis in HCORN cells (P < 0.05). Subconjunctival injection of purified MIP-133 in Chinese hamster eyes induced cytopathic effects resulting in corneal ulceration. Animals infected with A. castellanii-laden contact lenses and treated with AACOCF3 and CAY10650, showed significantly less severe keratitis as compared with control animals. Collectively, the results indicate that cPLA2α is involved in MIP-133 induced apoptosis of corneal epithelial cells, polymorphonuclear neutrophil infiltration, and production of CXCL2. Moreover, cPLA2α inhibitors can be used as a therapeutic target in Acanthamoeba keratitis


Related Products :
HS-173
HS-173
Price: 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
Y320
Y320
Price: 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
Tirasemtiv
Tirasemtiv
Price: 200mg, $659;500mg, $1150; 1g, $1595; 2g, $2355
N6022
N6022
Price: 200mg, $659;500mg, $1150; 1g, $1595; 2g, $2355
P7C3-A20
P7C3-A20
Price: 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
Rolapitant
Rolapitant
Price: 200mg, $950;500mg, $1695; 1g, $2490; 2g, $3590
XEN445
XEN445
Price: 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
Peramivir (RWJ 270201, BCX1812)
Peramivir (RWJ 270201, BCX1812)
Price: 200mg, $459;500mg, $850; 1g $1195; 2g, $1795