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XL041
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XL041图片
CAS NO:1256918-39-4
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品名称
BMS-852927
产品介绍

产品描述

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

体外活性

XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively)[1]. XL041 is potent, with an EC50=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA).

体内活性

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 3 mg/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 (0.1-3 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].

Cas No.

1256918-39-4

分子式

C29H28Cl2F2N2O4S

分子量

609.51

别名

BMS-852927

储存和溶解度

DMSO:100 mg/mL (164.07 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years