XL041 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

609.51

DMSO: 100mg/mL (164.07mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

C29H28Cl2F2N2O4S

OC(C)(C)C1=CN(C2=CC=C(C3=CC(S(=O)(C)=O)=C(CO)C(F)=C3)C=C2F)C(C(C)(C4=C(Cl)C=CC=C4Cl)C)=N1

1256918-39-4

LXRbeta

XL041 (BMS-852927) which has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. XL041 pre-treatment of C57BL/6J mice for 7 days results in potent, dose-dependent stimulation of cholesterol efflux in this system; reaching a maximum in the 3mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease[1].

Liver X Receptor; Others