tcsc2039 BMS-303141

BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC₅₀ value of 0.13 μM.

IC50 & Target: IC50: 0.13 uM (ACL)^[1]

In Vitro: 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^[1].

In Vivo: 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^[1].