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BMS-986169

Chemical Structure : BMS-986169

CAS No.: 1801151-08-5

BMS-986169 (BMS986169)

Catalog No.: PC-35166Not For Human Use, Lab Use Only.

BMS-986169 is a novel GluN2B negative allosteric modulator, demonstrates high binding affinity for the GluN2B allosteric site (Ki=4.0 nM) and selective inhibition of GluN2B receptor function (IC50=24 nM) in cells.

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    Biological Activity

    BMS-986169 is a novel GluN2B negative allosteric modulator, demonstrates high binding affinity for the GluN2B allosteric site (Ki=4.0 nM) and selective inhibition of GluN2B receptor function (IC50=24 nM) in cells.
    BMS-986169 shows negligible activity in an assay panel containing 40 additional pharmacological targets, and weakly inhibits hERG channel; produces a transient working memory impairment in monkeys.
    BMS-986169 does not produce ketamine-like hyperlocomotion or abnormal behaviors in mice or cynomolgus monkeys.

    Physicochemical Properties

    M.Wt 382.479
    Formula C23H27FN2O2
    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-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one

    References

    1. Marcin LR, et al. ACS Med Chem Lett. 2018 Apr 13;9(5):472-477.

    2. Bristow LJ, et al. J Pharmacol Exp Ther. 2017 Dec;363(3):377-393.

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