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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-AP-202
AP-202

Chemical Structure : AP-202

CAS No.: 2196197-89-2

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AP-202 (AP202)

货号: PC-72170Not For Human Use, Lab Use Only.

AP-202 (AP202) is a highly potent and selective α4β2 nAChR antagonist with binding Ki of 18 nM, 57-fold selectivity over α3β4 receptor.

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

    生物&药学活性

    AP-202 (AP202) is a highly potent and selective α4β2 nAChR antagonist with binding Ki of 18 nM, 57-fold selectivity over α3β4 receptor.
    AP-202 is agonist activity, also dispalys 40-fold, 10-fold and 90-fold selectivity over α4β4, α3β2, α3β4α5 receptors, does not activate α7 nAChR or block acetylcholine induced changes in membrane potential.
    AP-202 showed significant activity in blocking nicotine priming-induced as well as cue-induced reinstatement of nicotine seeking in vivo.

    物理化学性质&存储条件

    分子量 204.277
    分子式 C11H16N4
    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

    (S)-5-methyl-1-(2-(pyridin-3-yl)ethyl)imidazolidin-2-imine

    参考文献

    1. Jinhua Wu, et al. J Med Chem. 2017 Dec 28;60(24):10092-10104.

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