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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-NS-1209
NS-1209

Chemical Structure : NS-1209

CAS No.: 245063-59-6

NS-1209 (NS1209;SPD502)

货号: PC-61501Not For Human Use, Lab Use Only.

NS-1209 is a selective, water-soluble, in vivo long-lasting AMPA antagonist with Ki of 43 nM.

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

    生物&药学活性

    NS-1209 is a selective, water-soluble, in vivo long-lasting AMPA antagonist with Ki of 43 nM.
    NS-1209 display selectivity for the [3H] AMPA over the [3H]kainate- (IC50=81 uM), [3H]CGS19755, and [3H]glycine-binding sites (IC50 > 30 uM) in rat cortical membranes.
    NS-1209 inhibits AMPA-induced currents in cortical neurons with IC50 of 0.15 uM.
    NS-1209 blocks AMPA-evoked spike activity in rat hippocampus (ED50=6.1mg/kg).

    物理化学性质&存储条件

    分子量 516.57
    分子式 C24H28N4O7S
    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,Z)-2-(((5-(4-(N,N-dimethylsulfamoyl)phenyl)-8-methyl-2-oxo-1,2,6,7,8,9-hexahydro-3H-pyrrolo[3,2-h]isoquinolin-3-ylidene)amino)oxy)-4-hydroxybutanoic acid

    参考文献

    1. Nielsen EO, et al. J Pharmacol Exp Ther. 1999 Jun;289(3):1492-501.

    2. Erichsen HK, et al. Pain. 2002 Jul;98(1-2):151-61.

    3. Langer M, et al. Neuropharmacology. 2011 Oct-Nov;61(5-6):1033-47.

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