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XL041

Catalog No. T14679   CAS 1256918-39-4
Synonyms: BMS-852927

XL041 (BMS-852927) is an agonist of LXRβ-selective.

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XL041 Chemical Structure
XL041, CAS 1256918-39-4
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XL041 (BMS-852927) is an agonist of LXRβ-selective.
In vitro XL041 (BMS-852927) functions as an LXRβ-selective agonist, exhibiting 20% activity towards LXRα and 88% towards LXRβ relative to a comprehensive pan agonist in transactivation assays. Despite similar binding affinities to LXRα and LXRβ (19 and 12 nM, respectively)[1], XL041 proves to be potent, with an EC50 of 9 nM and achieves 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA).
In vivo XL041 (BMS-852927) exhibits a highly favorable efficacy profile at therapeutic doses in both cynomolgus monkeys and mice. In a distinct study, the compound effectively inhibited the progression of atherosclerosis over a 12-week period in LDLR knockout (KO) mice. Additionally, pre-treating C57BL/6J mice with XL041 for seven days induced a potent and dose-dependent increase in cholesterol efflux, peaking at a 70% enhancement over the control with a dose of 3 mg/kg/day. This effect was also observed in LDLR KO mice. Notably, the dosage range that inhibits atherosclerosis (0.1-3 mg/kg/day) aligns closely with the dosage range that stimulates macrophage reverse cholesterol transport (RCT) (0.03-3 mg/kg/day), indicating a conserved mechanism of action for LXR agonists in mitigating the disease.
Synonyms BMS-852927
Molecular Weight 609.51
Formula C29H28Cl2F2N2O4S
CAS No. 1256918-39-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (164.07 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Kirchgessner TG, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33.

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(20S)-Protopanaxatriol Gymnestrogenin GSK3987 T0901317 SR9243 GSK2033 BMS-779788 LXR-623

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Keywords

XL041 1256918-39-4 Metabolism Liver X Receptor BMS852927 BMS-852927 XL-041 XL 041 BMS 852927 inhibitor inhibit

 

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