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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-BMS-986169
BMS-986169

Chemical Structure : BMS-986169

CAS No.: 1801151-08-5

BMS-986169 (BMS986169)

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

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 382.479
    分子式 C23H27FN2O2
    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)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one

    参考文献

    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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