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GNE-616

Chemical Structure : GNE-616

CAS No.: 2244895-99-4

GNE-616 (GNE616;GNE 616)

Catalog No.: PC-36160Not For Human Use, Lab Use Only.

GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).

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

    Biological Activity

    GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).
    GNE-616 shows robust, concentration dependent reduction in nociceptive events with an EC50 of 740 nM.
    GNE-616 is a highly potent inhibitor of Nav1.7 in manual patch clamp electrophysiology assays (Kd=0.38 nM), showing >1000-fold selectivity over Nav1.1, Nav1.3, Nav1.4, and Nav1.5 and modest selectivity over Nav1.2 and Nav1.6 (30-70 fold).
    GNE-616 shows a robust PK/PD response in a Nav1.7 dependent mouse model.

    Physicochemical Properties

    M.Wt 537.534
    Formula C24H23F4N5O3S
    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)-6-fluoro-4-((2R,4S)-2-(pyridin-2-yl)-4-(trifluoromethyl)piperidin-1-yl)-N-(pyrimidin-4-yl)chromane-7-sulfonamide

    References

    1. McKerrall SJ, et al. J Med Chem. 2019 Apr 3. doi: 10.1021/acs.jmedchem.9b00141.

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