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首页-小分子抑制剂&激动剂-GPCR-mGluR-LY2812223
LY2812223

Chemical Structure : LY2812223

CAS No.: 1311385-20-2

LY2812223 (LY-2812223)

货号: PC-60818Not For Human Use, Lab Use Only.

LY2812223 is highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.

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

    生物&药学活性

    LY2812223 is highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.
    LY2812223 displays little to no affinity for mGlu1, mGlu4, mGlu5 or mGlu7 receptors.
    LY2812223 fully displaces the mGlu2/3 agonist radioligand [3H]LY459477 with Ki of 118 nM, inhibits forskolin-stimulated cAMP with EC50 of 16.1 nM.
    LY2812223 displays near maximal agonist responses at the mGlu2 receptor across all assay formats, while shows no functional agonist activity at the mGlu3 receptor except in the cAMP assay.

    物理化学性质&存储条件

    分子量 284.29
    分子式 C10H12N4O4S
    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

    (1R,2S,4R,5R,6R)-2-amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid

    参考文献

    1. Monn JA, et al. J Med Chem. 2015 Sep 24;58(18):7526-48.

    2. Felder CC, et al. J Pharmacol Exp Ther. 2017 Apr;361(1):190-197.

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