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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-INCB10820
INCB10820

Chemical Structure : INCB10820

CAS No.: 1310796-72-5

INCB10820 (PF-4178903;INCB 10820)

货号: PC-61576Not For Human Use, Lab Use Only.

INCB10820 (PF-4178903) is a potent, selective, orally bioavailable dual CCR2 and CCR5 antagonist with binding IC50 of 3.0 nM and 5.3 nM, respectively.

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

    生物&药学活性

    INCB10820 (PF-4178903) is a potent, selective, orally bioavailable dual CCR2 and CCR5 antagonist with binding IC50 of 3.0 nM and 5.3 nM, respectively.
    INCB10820 displays an IC50 of 4.3 nM in CCR5 chemotaxis functional assay.
    INCB10820 is active against mouse, rat and cynomolgus monkey CCR2 with binding IC50 of 2.8, 2.9 and 4.6 nM, respectively, but inactive against canine CCR2, also is active against mouse and cynomolgus monkey CCR5 with IC50 of 71 and 4.0 nM, respectively.

    物理化学性质&存储条件

    分子量 498.591
    分子式 C25H37F3N4O3
    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

    (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine

    参考文献

    1. Zheng C, et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6.

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