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AP-202

Chemical Structure : AP-202

CAS No.: 2196197-89-2

AP-202 (AP202)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 204.277
    Formula C11H16N4
    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

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

    References

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

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