XL652 是一种LXR的部分激动剂,能够作用于 LXRα (IC50:68 μM) 和 LXRβ (IC50:14 μM)。
产品描述
BMS-779788 is an LXRα/β partial agonist (IC50: 68/14 nM).
体外活性
BMS-779788 can effectively induce ATP binding transporters ABCA1 and ABCG1 in the human whole blood (EC50: 1.2 μM).
体内活性
BMS-779788 has an inducted effect of LXR target genes in blood in vivo (EC50: 610 nM). In elevating plasma triglyceride and LDL cholesterol, BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 respectively[1]. In mice, BMS-779788 displayed peripheral induction of ABCA1 at 3 and 10mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist[2].
Cas No.
918348-67-1
分子式
C28H29ClN2O3S
分子量
509.06
别名
XL 652;XL-652;BMS-788;XL652;EXEL04286652
储存和溶解度
DMSO:31 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years