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GX-936

Chemical Structure : GX-936

CAS No.: 1235406-09-3

GX-936 (GX936;PF 05196233)

Catalog No.: PC-62324Not For Human Use, Lab Use Only.

GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the 1KαPMTX-evoked N1742K response with IC50 of 40 nM.

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    Biological Activity

    GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the 1KαPMTX-evoked N1742K response with IC50 of 40 nM.
    GX-936 inhibits Nav1.7 through a voltage-sensor trapping mechanism, likely by stabilizing inactivated states of the channel.

    Physicochemical Properties

    M.Wt 575.585
    Formula C24H20F3N7O3S2
    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

    3-Cyano-4-[2-[1-(1-ethyl-3-azetidinyl)-1H-pyrazol-5-yl]-4-(trifluoromethyl)phenoxy]-N-1,2,4-thiadiazol-5-yl-benzenesulfonamide

    References

    1. Ahuja S, et al. Science. 2015 Dec 18;350(6267):aac5464.

    2. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801.

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