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首页-小分子抑制剂&激动剂-Others-Other Targets-F12511
F12511

Chemical Structure : F12511

CAS No.: 202340-45-2

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F12511 (Eflucimibe)

货号: PC-49562Not For Human Use, Lab Use Only.

Eflucimibe (F12511) is a highly potent, selective inhibitor of acyl-CoA: cholesterol acyltransferase ( ACAT/SOAT) with IC50 of 3, 7, and 71 nM in whole cell assays using HepG2, CaCo-2 and THP-1 cell lines, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Eflucimibe (F12511) is a highly potent, selective inhibitor of acyl-CoA: cholesterol acyltransferase ( ACAT/SOAT) with IC50 of 3, 7, and 71 nM in whole cell assays using HepG2, CaCo-2 and THP-1 cell lines, respectively.
    F 12511 potently inhibits ACAT activity in microsomal preparations from various animal species as well as of cholesterol esterification in relevant human cell lines in culture.
    F 12511 inhibits ACAT activity in microsomal preparations with EC values ranged from 41 nM for hypercholesterolemic rabbit intestine to 223 nM for normocholesterolemic hamster liver.
    Orally administered F 12511 displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (rat, guinea-pig, rabbit), reduced plasma cholesterol levels in guinea-pigs with ED30 of 0.008 mg/kg.
    F 12511 lowered plasma cholesterol levels in New Zealand rabbits fed a cholesterol-free casein-rich diet.

    物理化学性质&存储条件

    分子量 469.728
    分子式 C29H43NO2S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (S)-2',3',5'-trimethyl-4'-hydroxy-alpha-dodecylthio-alpha-phenylacetanilide

    参考文献

    1. Junquero D, et al. Biochem Pharmacol. 2001 Jan 1;61(1):97-108.

    2. Junquero D, et al. Atherosclerosis. 2001 Mar;155(1):131-42.

    3. Zamorano-León JJ, et al. J Cardiovasc Pharmacol. 2006 Sep;48(3):128-34.

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