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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-AMG8379
AMG8379

Chemical Structure : AMG8379

CAS No.: 1642112-31-9

AMG8379 (AMG-8379)

货号: 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.

规格 价格 库存 数量
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 543.926
    分子式 C25H16ClF2N3O5S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

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

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