Name: Ezetimibe
Price: 228.00 USD

- Overview
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    Background
    
    Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1].
    Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones.
    In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin, lycopene and lutein:zeaxanthin(1:1). At the same time, ezetimibe inhibited cholesterol transport by 31%. Ezetimibe decreased the expression of the surface receptors SR-BI, ATP binding cassette transporter, subfamily A (ABCA1), Niemann-Pick type C1 Like 1 protein (NPC1L1) and retinoid acid receptor (RAR)γ, sterol-regulatory element binding proteins SREBP-1 and SREBP-2, and liver X receptor (LXR)β [3].
    In apolipoprotein E knockout (apoE-/-) mice, ezetimibe (3 mg/kg) inhibited cholesterol absorption by 90%. Ezetimibe reduced plasma cholesterol, increased HDL levels, and inhibits the progression of atherosclerosis [1]. In phase III human trials, Ezetimibe (10 mg) significantly reduced the levels of LDL cholesterol, total cholesterol and triglycerides and increased the level of HDL cholesterol [2].
    
    [1]. Davis HR Jr, Compton DS, Hoos L, et al. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice. Arterioscler Thromb Vasc Biol, 2001, 21(12): 2032-2038.
    [2]. Clader JW. The discovery of ezetimibe: a view from outside the receptor. J Med Chem, 2004, 47(1): 1-9.
    [3]. During A, Dawson HD, Harrison EH. Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr, 2005, 135(10): 2305-2312.
- Properties
  - Alternative Name
    
    (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
    
    CAS Number
    
    163222-33-1
    
    Molecular Formula
    
    C24H21F2NO3
    
    Molecular Weight
    
    409.4
    
    Appearance
    
    A solid
    
    Purity
    
    99.90%
    
    Solubility
    
    ≥20.45 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Ezetimibe

Ezetimibe

Background

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