| Bioactivity | BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 μM. | ||||||||||||
| Target | IC50: 0.13 uM (ACL) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | BMS-303141 | ||||||||||||
| CAS | 943962-47-8 | ||||||||||||
| Formula | C19H15Cl2NO4S | ||||||||||||
| Molar Mass | 424.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |