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AMG 8379

Chemical Structure : AMG 8379

CAS No.: 1642112-31-9

AMG 8379 (AMG-8379;AMG8379)

Catalog No.: PC-60629Not For Human Use, Lab Use Only.

AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.

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

    Biological Activity

    AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.
    AMG 8379 potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays.
    AMG 8379 displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5.
    AMG 8379 blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking.
    AMG 8379 exhibits pharmacodynamic effects in translatable models of both itch and pain.

    Physicochemical Properties

    M.Wt 543.926
    Formula C25H16ClF2N3O5S
    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

    (P)-1-(3'-chloro-2,5'-difluoro-5-methoxy-4-biphenylyl)-N-3-isoxazolyl-2-oxo-1,2-dihydro-6-quinolinesulfonamide

    References

    1. Kornecook TJ, et al. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160.

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