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GluN2A PAM (R)-9

Chemical Structure : GluN2A PAM (R)-9

CAS No.:

GluN2A PAM (R)-9 (GluN2A positive allosteric modulator (R)-9)

Catalog No.: PC-20368Not For Human Use, Lab Use Only.

GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%.

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    Biological Activity

    GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%.
    GluN2A PAM (R)-9 shows good NMDA-subtype selectivity, with>59-fold selectivity for GluN2B and 2C and 19-fold selectivity for GluN2D in the Ca2+ influx assay using CHO cells.
    GluN2A PAM (R)-9 (10 mg/kg) significantly enhances long-term potentiation in the rat hippocampus 24 h after oral administration.

    Physicochemical Properties

    M.Wt 380.78
    Formula C16H15ClF2N6O
    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

    (R)-3-(2-((5-Chloro-3-(difluoromethyl)-1H-pyrazol-1-yl)methyl)-7-methyl-4-oxopyrazolo[1,5-a]pyrazin-5(4H)-yl)butanenitrile

    References

    1. Sakurai F, et al. Bioorg Med Chem. 2022 Feb 15;56:116576.

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