BMS-779788

BMS-779788CAS号: 918348-67-1分子式: C28H29ClN2O3S分子量: 508.15描述纯度储存/保存方法别名外观靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
BMS-779788(XL652) is a novel small-molecule modulator of the Liver X Receptor (LXR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic disorders.
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
BMS-779788; BMS 779788; BMS779788; BMS-788; BMS 788; BMS788; XL-652; XL652; XL652; EXEL 04286652; EXEL04286652; EXEL-04286652
外观
Powder
生物活性
靶点
LXR
In vitro(体外研究)
The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2 μM, 55% efficacy).
In vivo(体内研究)
BMS-779788 induces LXR target genes in blood in vivo with an EC50=610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B. In mice BMS-779788 displays peripheral induction of ABCA1 at 3 and 10 mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist.

分子结构图

BMS-779788