BMS-852927

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

一种新型有效的部分 LXRβ 选择性激动剂 (EC50=9 nM)，与反式激活测定中的全泛激动剂相比，具有 20% LXRα 和 88% LXRβ 活性。

A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays; has EC50 of 9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay, has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively; increases reverse cholesterol transport pathways in clinical trials.

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

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.

BMS 852927 | BMS852927 | XL041 | XL-041

Nuclear Receptor/Transcription Factor

LXR

LXR

Cardiovascular Disease

Hypercholesterolemia

1256918-39-4

609.51

C29H28Cl2F2N2O4S

>98% (HPLC)

DMSO : ≥ 150 mg/mL246.10 mM

CC(C)(C1=CN(C(=N1)C(C)(C)C2=C(C=CC=C2Cl)Cl)C3=C(C=C(C=C3)C4=CC(=C(C(=C4)S(=O)(=O)C)CO)F)F)O

2-(2-(2-(2,6-dichlorophenyl)propan-2-yl)-1-(3,3′-difluoro-4′-(hydroxymethyl)-5′-(methylsulfonyl)biphenyl-4-yl)-1H-imidazol-4-yl)propan-2-ol

(-20℃)

With Ice Pack

≥ 2 years