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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Monoacylglycerol Lipase (MAGL)-ABX-1431 hydrochloride
ABX-1431 hydrochloride

Chemical Structure : ABX-1431 hydrochloride

CAS No.: 2043074-64-0

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ABX-1431 hydrochloride (ABX1431, Elcubragistat)

货号: PC-35551Not For Human Use, Lab Use Only.

ABX-1431 (Elcubragistat) hydrochloride is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MAGL) with IC50 of 14 nM (hMAGL).

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

    生物&药学活性

    ABX-1431 (Elcubragistat) hydrochloride is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MAGL) with IC50 of 14 nM (hMAGL).
    ABX-1431 displays 23-fold selectivity for MGLL versus ABHD6 and CES1c, as well as exquisite selectivity of against other members of the serine hydrolase class.
    ABX-1431 inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model.

    物理化学性质&存储条件

    分子量 543.859
    分子式 C20H23ClF9N3O2
    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

    1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate hydrochloride

    参考文献

    1. Cisar JS, et al. J Med Chem. 2018 Aug 1. doi: 10.1021/acs.jmedchem.8b00951.

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