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NCATS-SM7270

Chemical Structure : NCATS-SM7270

CAS No.:

NCATS-SM7270

Catalog No.: PC-49686Not For Human Use, Lab Use Only.

NCATS-SM7270 is a specific small molecule NADPH oxidase 2 (NOX2) inhibitor with IC50 of 2.1 uM (Polymorphonuclear leukocytes, PMN), inhibits NOX2 in primary human and mouse granulocytes.

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    Biological Activity

    NCATS-SM7270 is a specific small molecule NADPH oxidase 2 (NOX2) inhibitor with IC50 of 2.1 uM (Polymorphonuclear leukocytes, PMN), inhibits NOX2 in primary human and mouse granulocytes.
    NCATS-SM7270 exhibited improved permeability, solubility, and half-life in rat microsomes, which retained similar activity against human neutrophil NOX2 and lower activity against xanthine oxidase compared to GSK2795039.
    NCATS-SM7270 displayed no detectable activity against NOX3 and NOX4, and only marginal activity at the highest dose tested (about 100x the IC50 versus NOX2) against NOX1 and NOX5.
    NCATS-SM7270 specifically inhibited NOX2 and had reduced inhibitory activity against xanthine oxidase in vitro.
    NCATS-SM7270 protected mice from mild traumatic brain injury, partially reversed mild traumatic brain injury (mTBI) in NOX4KO mice.

    Physicochemical Properties

    M.Wt 446.53
    Formula C23H22N6O2S
    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

    N-(1-cyclopropyl-3-(1-methyl-1H-indol-6-yl)-1H-pyrrolo [2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide

    References

    1. Hannah Mason, et al. Redox Biol. 2023 Jan 18;60:102611.

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