BMS-303141

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

BMS-303141 是一种有效的 ATP-柠檬酸裂解酶 (ACL) 抑制剂（IC50：0.13 uM，人重组 ACL）。

BMS303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS-303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.

In HepG2 cells, BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM. BMS-303141 shows no cytotoxicity up to 50 lM under a cell based Alamar Blue cytotoxicity assay, indicating the observed inhibition of lipid synthesis is not a result of compound-induced cytotoxicity.

Chronic oral dosing of BMS-303141 in high-fat fed mice lowers approximate 20-30% plasma cholesterol and triglycerides, as well as 30-50% fasting plasma glucose. Chronic treatment with BMS-303141 shows a gradual inhibition of weight gain along with a reduction in adiposity without apparent changes in food intake. BMS-303141 shows an oral bioavailability of 55% but a relatively short half-life of 2.1 h.

BMS303141 | BMS-303141 | BMS 303141

Endocrinology/Hormones

AChR

ACL

Metabolic Disease

——

943962-47-8

424.3

C19H15Cl2NO4S

>98% (HPLC)

DMSO : ≥ 47 mg/mL; 110.77 mM

c1c(cccc1)c1cc(c(cc1)OC)NS(=O)(=O)c1c(O)c(cc(c1)Cl)Cl

3,5-Dichloro-2-hydroxy-N-(4-methoxy[1,1′-biphenyl]-3-yl)-benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years