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首页-小分子抑制剂&激动剂-GPCR-mGluR-BMS-984923
BMS-984923

Chemical Structure : BMS-984923

CAS No.: 1375752-78-5

BMS-984923 (BMS984923, BMS 984923)

货号: PC-35962Not For Human Use, Lab Use Only.

BMS-984923 (BMS 984923) is a potent silent allosteric modulator (SAM) of mGluR5 with competitive antagonism of MPEPy binding with Ki of 0.6 nM, but has no detectable agonist and antagonist activity at mGluR5 signaling.

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

    生物&药学活性

    BMS-984923 (BMS 984923) is a potent silent allosteric modulator (SAM) of mGluR5 with competitive antagonism of MPEPy binding with Ki of 0.6 nM, but has no detectable agonist and antagonist activity at mGluR5 signaling.
    BMS-984923 does not affect glutamate/DHPG ((S)-3,5-Dihydroxyphenylglycine)-induced Ca2+ signaling in mGluR5-overexpressing HEK293T cells and cultured nureons.
    BMS-984923 reduces the interaction of PrPC with mGluR5 in membrane fractions, prevents Aβo-induced signal transduction in brain slices, and rescues memory deficits and synaptic depletion in the APPswe/PS1ΔE9 transgenic mouse brain.

    物理化学性质&存储条件

    分子量 374.824
    分子式 C22H15ClN2O2
    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

    2-Oxazolidinone, 5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)-3-pyridinyl]-, (4R,5R)-

    参考文献

    1. Huang H, et al. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9.

    2. Haas LT, et al. Cell Rep. 2017 Jul 5;20(1):76-88.

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