BMS-779788

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、高选择性的 LXR 部分激动剂，对 LXRβ 的 Ki 值为 14 nM。

A potent, highly selective partial LXR agonist with Ki of 14 nM for LXRβ, shows moderate selectivity (5-fold) over LXRα (Ki=68 nM); only has activity for PXR (ECU0=2 uM) in a panel of 14 NHRs; induces LXR target genes in blood in vivo (EC50=610 nM); increases in biliary cholesterol and decreases in phospholipid and bile acid in animal models.Atherosclerosis Phase 1 Clinical(In Vitro):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):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.

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).

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.

XL-652 | BMS-788 | EXEL-04286652

Nuclear Receptor/Transcription Factor

LXR

LXRα|LXRβ

Cardiovascular Disease

Atherosclerosis

918348-67-1

509.0594

C28H29ClN2O3S

>98% (HPLC)

DMSO: ≥ 31 mg/mL

CC(C)(C1=CC=CC=C1Cl)C2=NC(=CN2C3=CC=C(C=C3)C4=CC(=CC=C4)S(=O)(=O)C)C(C)(C)O

1H-Imidazole-4-methanol, 2-[1-(2-chlorophenyl)-1-methylethyl]-α,α-dimethyl-1-[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]-

(-20℃)

With Ice Pack

≥ 2 years