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NaV1.7 inhibitor 51

Chemical Structure : NaV1.7 inhibitor 51

CAS No.: 2244153-85-1

NaV1.7 inhibitor 51

Catalog No.: PC-72207Not For Human Use, Lab Use Only.

NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).

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    Biological Activity

    NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).
    NaV1.7 inhibitor 51 shows good selectivity against other NaV isoforms and minimal inhibition at 10 uM for the resting state across different NaV isoforms.
    NaV1.7 inhibitor 51 exhibits state-dependent block of human, monkey, and mouse NaV1.7 with a similar potency range.
    NaV1.7 inhibitor 51 shows significant effects on the CCI-induced neuropathic pain model.

    Physicochemical Properties

    M.Wt 499.512
    Formula C24H20F3N5O2S
    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

    (S)-1-(2-(1-methyl-1H-pyrazol-5-yl)-4-(trifluoromethyl)phenyl)-N-(pyrimidin-2-yl)-2,3-dihydro-1H-indene-5-sulfonamide

    References

    1. Vidya Ramdas, et al. J Med Chem. 2020 Jun 11;63(11):6107-6133.

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