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INCB10820

Chemical Structure : INCB10820

CAS No.: 1310796-72-5

INCB10820 (PF-4178903;INCB 10820)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 498.591
    Formula C25H37F3N4O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

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

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