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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cytochrome P450 (CYPs)-LKY-047
LKY-047

Chemical Structure : LKY-047

CAS No.: 1954681-29-8

LKY-047 (LKY047)

货号: PC-20617Not For Human Use, Lab Use Only.

LKY-047 (LKY047) is a potent, highly selective and reversible competitive cytochrome P450 CYP2J2 (CYP2J2) inhibitor with IC50 of 1.7 uM.

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

    生物&药学活性

    LKY-047 (LKY047) is a potent, highly selective and reversible competitive cytochrome P450 CYP2J2 (CYP2J2) inhibitor with IC50 of 1.7 uM.
    LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 and 2.61 μM, respectively.
    LKY-047 also acts as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a Ki value of 3.61 μM.
    LKY-047 displays no inhibitory effect on other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A (IC50 > 50 uM).
    LKY-047 is useful as a selective CYP2J2 inhibitor in P450 reaction phenotyping studies and the biologic function study of this enzyme.

    物理化学性质&存储条件

    分子量 421.41
    分子式 C23H19NO7
    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)-8,8-dimethyl-2-oxo-7,8-dihydro-2H,6H-pyrano[3,2-g]chromen-7-yl (E)-3-(4-nitrophenyl)acrylate

    参考文献

    1. Nguyen Minh Phuc, et al. Drug Metab Dispos. 2017 Jul;45(7):765-769.

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