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BMS-751324

Chemical Structure : BMS-751324

CAS No.: 948842-66-8

BMS-751324 (BMS751324)

Catalog No.: PC-63564Not For Human Use, Lab Use Only.

BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM.
    BMS-751324 is effectively bioconverted into parent drug BMS-582949 in vivo by alkaline phosphatase and esterase in a stepwise manner.
    BMS-751324 demonstrates similar efficacy in rat LPS-induced TNFα pharmacodynamic model and rat adjuvant arthritis model compared with BMS-582949.
    BMS-751324 is indeed effective in addressing the pH-dependent absorption issue associated with BMS-582949.

    Physicochemical Properties

    M.Wt 694.638
    Formula C32H35N6O10P
    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

    (((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyl)oxy)methyl 2-(4-(phosphonooxy)phenyl)acetate

    References

    1. Liu C, et al. J Med Chem. 2015 Oct 8;58(19):7775-84.

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