| Description | BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL). |
| In vitro | 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]. |
| 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 exhibits an oral bioavailability of 55% while a relatively short half-life of 2.1 h[1]. |
| Target activity | ACL:0.13 μM |
| Synonyms | BMS 303141 |
| molecular weight | 424.3 |
| Molecular formula | C19H15Cl2NO4S |
| CAS | 943962-47-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (129.63 mM) |
| References | 1. Li JJ, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. |
| Citations | 1. Tang C, Wang H, Guo L, et al.CpG-Conjugated Silver Nanoparticles as a Multifunctional Nanomedicine to Promote Macrophage Efferocytosis and Repolarization for Atherosclerosis Therapy.ACS Applied Materials & Interfaces.2023 |