BMS-303141

• CAT Number: I005616
• CAS Number: 943962-47-8
• Molecular Formula: C₁₉H₁₅Cl₂NO₄S
• Molecular Weight: 424.3
• Purity: ≥95%
• Synonyms: BMS303141;BMS 303141
• Target: ATP citrate lyase
• Solubility: DMSO: ≥ 47 mg/mL
• Storage: Store at -20C
• IC50: 0.13 uM
• InChI: InChI=1S/C19H15Cl2NO4S/c1-26-17-8-7-13(12-5-3-2-4-6-12)9-16(17)22-27(24,25)18-11-14(20)10-15(21)19(18)23/h2-11,22-23H,1H3
• InChIKey: SIIPNDKXZOTLEA-UHFFFAOYSA-N
• SMILES: COC1=C(C=C(C=C1)C2=CC=CC=C2)NS(=O)(=O)C3=CC(=CC(=C3O)Cl)Cl

BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor with IC50 value of 0.13 uM (human recombinant ACL). 


in vitro: In HepG2 cells, BMS-303141 showed inhibition of total lipid syntheses with an IC50 of 8 μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, BMS-303141 showed no cytotoxicity up to 50 μM, indicating the observed inhibition of lipid synthesis was not a result of compound-induced cytotoxicity [1]. 


in vivo: In mice, BMS-303141 showed an oral bioavailability of 55% but a relatively short half-life of 2.1 h.20 We therefore decided to dose BMS-303141 admixed in the food to assure greater duration of exposure in subsequent chronic efficacy studies.There were a total of four groups in the study; mice on normal diet and high-fat diet controls, and two treated groups that were supplemented with BMS-303141 in their high-fat diet to an equivalent daily dose of 10 or 100 mg/kg. The study was continued for a total of 34 days. Food consumption and body weight gain were tracked along with weekly assessment of lipid and glucose plasma chemistries [1].

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.