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首页-小分子抑制剂&激动剂-GPCR-mGluR-AZD8529 mesylate
AZD8529 mesylate

Chemical Structure : AZD8529 mesylate

CAS No.: 1314217-69-0

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AZD8529 mesylate (AZD 8529 mesylate)

货号: PC-63181Not For Human Use, Lab Use Only.

AZD8529 mesylate is a potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes.

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

    生物&药学活性

    AZD8529 mesylate is a potent, selective mGluR2 positive allosteric modulator with EC50 of 195 nM, does not produce any positive allosteric modulator responses for mGluR1 and 3-8 subtypes.
    AZD8529 potentiates agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus and striatum.
    AZD8529 decreases nicotine self-administration at doses (0.3-3 mg/kg) in monkeys, also reduces nicotine priming- and cue-induced reinstatement of nicotine seeking, decreases nicotine-induced accumbens dopamine release in rats.

    物理化学性质&存储条件

    分子量 583.583
    分子式 C25H28F3N5O6S
    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

    7-methyl-5-(3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl)-2-(4-(trifluoromethoxy)benzyl)isoindolin-1-one methanesulfonate

    参考文献

    1. Justinova Z, et al. Biol Psychiatry. 2015 Oct 1;78(7):452-62.

    2. Caprioli D, et al. Biol Psychiatry. 2015 Oct 1;78(7):463-73.

    3. Li X, et al. Psychopharmacology (Berl). 2016 May;233(10):1801-14.

    4. Augier E, et al. Neuropsychopharmacology. 2016 Nov;41(12):2932-2940.

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