BMS303141是高效性和可渗透细胞的ACL抑制剂(IC50:0.13 μM)。
产品描述
BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL).
体外活性
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].
体内活性
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].
Cas No.
943962-47-8
分子式
C19H15Cl2NO4S
分子量
424.29
别名
BMS 303141
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years