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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-INCB9471
INCB9471

Chemical Structure : INCB9471

CAS No.: 869769-98-2

INCB9471 (INCB 9471;INCB-9471)

货号: PC-60672Not For Human Use, Lab Use Only.

INCB9471 is a potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.

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

    生物&药学活性

    INCB9471 is a potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.
    INCB9471 inhibits CCR5-mediated signaling events such as intracellular calcium mobilization, ERK phosphorylation, and CCR5 receptor internalization with IC50 values of 16, 3, and 1.5 nM, respectively.
    INCB9471 demonstrates anti-HIV-1 activity against R5 HIV-1 strains representing the major clades including A, B, C, D, E, F, G, and J with mean IC50 of 9 nM in PBMCs.
    INCB9471 also is a potent inhibitor of mutant HIV-1 variants that are resistant to other drugs including NRTIs, NNRTIs, PIs, and the fusion inhibitor T20.

    物理化学性质&存储条件

    分子量 559.678
    分子式 C30H40F3N5O2
    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

    (4,6-dimethylpyrimidin-5-yl)(4-((S)-4-((1R,2R)-2-ethoxy-5-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)-3-methylpiperazin-1-yl)-4-methylpiperidin-1-yl)methanone

    参考文献

    1. Xue CB, et al. ACS Med Chem Lett. 2010 Aug 25;1(9):483-7.

    2. Shin N, et al. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39.

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