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GPR52 antagonist E7

Chemical Structure : GPR52 antagonist E7

CAS No.: 2305684-39-1

GPR52 antagonist E7 (AD31E7)

货号: PC-72129Not For Human Use, Lab Use Only.

GPR52 antagonist E7 is a novel Gpr52 antagonist, shows significant inhibitory effect on WO-459 (100 nM)-induced cAMP elevation in HEK293/GPR52 cells with IC50 of 12.0 uM.

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

    生物&药学活性

    GPR52 antagonist E7 is a novel Gpr52 antagonist, shows significant inhibitory effect on WO-459 (100 nM)-induced cAMP elevation in HEK293/GPR52 cells with IC50 of 12.0 uM.
    GPR52 antagonist E7 did not block cAMP elevation induced by Gαs-coupled GPCRs, including β2AR, GCGR and GLP-1R.
    GPR52 antagonist E7 reduces mutant HTT levels and rescues Huntington's disease-associated phenotypes in cellular and mouse models.
    GPR52 antagonist E7 acts as an tntracellular covalent ligand of orphan receptor GPR52.

    物理化学性质&存储条件

    分子量 358.39
    分子式 C20H22O6
    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

    (3aR,4S,6Z,11E,12aR)-11-methyl-3-methylene-2,7-dioxo-2,3,3a,4,5,9,10,12a-octahydro-7H-6,9-(metheno)furo[2,3-f][1]oxacycloundecin-4-yl (Z)-2-methylbut-2-enoate

    参考文献

    1. Song H, et al. Brain. 2018 Jun 1;141(6):1782-1798.

    2. Ma M, et al. ACS Chem Biol. 2020 Dec 18;15(12):3275-3284.

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