BMS303141是高效性和可渗透细胞的ACL抑制剂(IC50:0.13 μM)。

BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL).

BMS-303141 shows inhibition of total lipid syntheses with an IC50 of 8 μM in HepG2 cells. 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[1].

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 exhibits an oral bioavailability of 55% while a relatively short half-life of 2.1 h[1].

943962-47-8

C19H15Cl2NO4S

424.29

BMS 303141

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years