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首页-小分子抑制剂&激动剂-GPCR-mGluR-LY3020371 hydrochloride
LY3020371 hydrochloride

Chemical Structure : LY3020371 hydrochloride

CAS No.: 1377615-44-5

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LY3020371 hydrochloride (LY-3020371 hydrochloride)

货号: PC-60730Not For Human Use, Lab Use Only.

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.

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

    生物&药学活性

    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.
    LY3020371 exhibits little to no agonist or antagonist activity against mGlu1/4/5/6/7/8 (>1 uM potenct).
    LY3020371 potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation with IC50 of 16.2 nM, blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50= 34 nM) and in an intact hippocampal slice preparation (IC50= 46 nM).
    LY3020371 exerts an antidepressant-like signature in vivo.

    物理化学性质&存储条件

    分子量 395.802
    分子式 C15H16ClF2NO5S
    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

    (1S,2R,3S,4S,5R,6R)-2-amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid hydrochloride

    参考文献

    1. Chappell MD, et al. J Med Chem. 2016 Dec 22;59(24):10974-10993.

    2. Witkin JM, et al. Neuropharmacology. 2017 Mar 15;115:100-114.

    3. Witkin JM, et al. J Pharmacol Exp Ther. 2017 Apr;361(1):68-86.

    4. Witkin JM, et al. Pharmacol Biochem Behav. 2017 Apr;155:43-55.

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