BMS-303141

- Overview
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    Background
    
    BMS-303141 is a potent inhibitor of ATP-citrate lyase with IC50 value of 0.13 μM [1].
    ATP-citrate lyase (ACL) is a cytosolic enzyme that responsible for the production of cytosolic acetyl-CoA, a precursor required for de novo biosyntheses of cholesterol and fatty acids. Inhibition of ACL is used to treat dyslipidemia and obesity [1].
    BMS-303141 is a potent ATP-citrate lyase inhibitor. In HepG2 cells, BMS-303141 inhibited total lipid syntheses with IC50 value of 8 μM. Also, BMS-303141 showed no cytotoxicity up to 50 μM [1].
    In mice, BMS-303141 exhibited an oral bioavailability of 55%. In high-fat fed mice, BMS-303141 reduced the levels of plasma triglyceride, cholesterol by 20-30% and glucose by 30-50% and inhibited weight gain [1]. BMS-303141 inhibited ACL with IC50 value of 0.94 μM for human ACL in a concentration dependant way [2].
    
    [1]. Li JJ, Wang H, Tino JA, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett, 2007, 17(11): 3208-3211.
    [2]. Ma Z, Chu CH, Cheng D. A novel direct homogeneous assay for ATP citrate lyase. J Lipid Res, 2009, 50(10): 2131-2135.
- Properties
  - Alternative Name
    
    3,5-dichloro-2-hydroxy-N-(4-methoxy-[1,1'-biphenyl]-3-yl)benzenesulfonamide
    
    CAS Number
    
    943962-47-8
    
    Molecular Formula
    
    C19H15Cl2NO4S
    
    Molecular Weight
    
    424.3
    
    Appearance
    
    A solid
    
    Purity
    
    99.51%
    
    Solubility
    
    ≥21.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BMS-303141

Background

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