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LY2812223

Chemical Structure : LY2812223

CAS No.: 1311385-20-2

LY2812223 (LY-2812223)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 284.29
    Formula C10H12N4O4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

    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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