BMS-852927
BMS-852927 Basic information
- Product Name:
- BMS-852927
- Synonyms:
-
- BMS-852927
- 2-(2-(2-(2,6-dichlorophenyl)propan-2-yl)-1-(3,3'-difluoro-4'-(hydroxymethyl)-5'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-4-yl)propan-2-ol
- BMS-852927 (BMS 852927
- XL041
- XL-041)
- 1H-Imidazole-4-methanol, 2-[1-(2,6-dichlorophenyl)-1-methylethyl]-1-[3,3'-difluoro-4'-(hydroxymethyl)-5'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]-α,α-dimethyl-
- XL041（BMS-852927）
- XL041,XL-041
- CAS:
- 1256918-39-4
- MF:
- C29H28Cl2F2N2O4S
- MW:
- 609.51
- Mol File:
- 1256918-39-4.mol
BMS-852927 Chemical Properties
- Boiling point:
- 810.6±75.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 150 mg/mL (246.10 mM)
- form
- Solid
- pka
- 11.20±0.10(Predicted)
- color
- White to off-white
BMS-852927 Usage And Synthesis
Uses
XL041 (BMS-852927) is an LXRβ-selective agonist.
in vivo
XL041 (BMS-852927), has a very favorable profile at efficacious doses in cynomolgus monkeys and 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 3 mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3 mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3 mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease[1].
References
[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. DOI:10.1016/j.cmet.2016.07.016
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