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

Chemical Structure : ABX-1431

CAS No.: 1446817-84-0

ABX-1431 (ABX1431, Elcubragistat)

货号: PC-35522Not For Human Use, Lab Use Only.

Elcubragistat (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MAGL) with IC50 of 14 nM (hMAGL).

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100 mg ¥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Elcubragistat (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MAGL) with IC50 of 14 nM (hMAGL).
Elcubragistat (ABX1431) displays 23-fold selectivity for MGLL versus ABHD6 and CES1c, as well as exquisite selectivity of against other members of the serine hydrolase class.
Elcubragistat (ABX1431) 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 507.401
分子式 C20H22F9N3O2
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)phenyl]methyl]piperazine-1-carboxylate

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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