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GRN-529

Chemical Structure : GRN-529

CAS No.: 1253291-12-1

GRN-529 (GRN 529, GRN529)

货号: PC-61060Not For Human Use, Lab Use Only.

GRN-529 is a highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.

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

    生物&药学活性

    GRN-529 is a highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.
    GRN-529 displays >1,000-fold selective vs mGluR1.
    GRN-529 reduces repetitive behaviors and rescues social deficits in mouse models of autism, demonstrates dose-dependent efficacy across a therapeutically relevant battery of animal models, comprising depression, anxiety and pain, with no effect on rat sexual behavior or motor co-ordination.

    物理化学性质&存储条件

    分子量 391.378
    分子式 C22H15F2N3O2
    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

    (4-(difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-yl)methanone

    参考文献

    1. Silverman JL, et al. Sci Transl Med. 2012 Apr 25;4(131):131ra51.

    2. Hughes ZA, et al. Neuropharmacology. 2013 Mar;66:202-14.

    3. Harvey BD, et al. Neuropharmacology. 2013 Dec;75:19-30.

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