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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-NBI-921352
NBI-921352

Chemical Structure : NBI-921352

CAS No.: 2154408-63-4

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NBI-921352 (XEN901, NBI 921352)

货号: PC-72850Not For Human Use, Lab Use Only.

NBI-921352 (XEN901, NBI 921352) is a potent, highly selective, orally active inhibitor of NaV1.6 with IC50 of 51 nM (hNaV1.6 channel currents inhibition).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    NBI-921352 (XEN901, NBI 921352) is a potent, highly selective, orally active inhibitor of NaV1.6 with IC50 of 51 nM (hNaV1.6 channel currents inhibition).
    NBI-921352 displays selectivity ratios for hNaV1.6 versus the other hNaV isoforms (IC50 hNaV1.X / IC50 hNaV1.6) of 756 (NaV1.1), 134 (NaV1.2), 276 (NaV1.7) and >583 (NaV1.3, NaV1.4, NaV1.5).
    NBI-921352 is a state-dependent inhibitor, preferentially inhibiting inactivatedchannels.
    NBI-921352 demonstrated action-potential firing in glutamatergic excitatory pyramidal neurons, while sparing fast-spiking inhibitory interneurons, where NaV1.1 predominates.
    Oral administration of NBI-921352 prevented electrically induced seizures in a Scn8a GoF mouse, as well as in wild-type mouse and rat seizure models.
    NBI-921352 is more potent than three commonly sodium channel inhibitor anti-seizure medicines (carbamazepine, phenytoin, and lacosamide).

    物理化学性质&存储条件

    分子量 460.586
    分子式 C22H25FN4O2S2
    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

    (R)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2-fluoro-5-methyl-N-(thiazol-4-yl)benzenesulfonamide

    参考文献

    1. J P Johnson, et al. Elife. 2022 Mar 2;11:e72468.

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