Catalog Number: 5206
Chemical Name: 4-[Bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl]-1H-1,2,4-triazol-1-yl-methanone
Biological Activity
Potent and selective monoacylglycerol lipase (MAGL) inhibitor (IC50 = 0.4 nM). Exhibits >13,000 and ~630-fold selectivity for MAGL over FAAH and ABHD6, respectively. Increases brain levels of 2-arachidonoylglycerol (2-AG) levels in mice in vivo. Promotes analgesia in pain models.
Technical Data
  • M.Wt:
    434.44
  • Formula:
    C23H22N4O5
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1515855-97-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase.
    Aaltonen et al.
    Chem.Biol., 2013;20:379
  2. Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency.
    Laitinen et al.
    Mol.Pharmacol., 2014;85:510
  3. In vivo characterization of the ultrapotent monoacylglycerol lipaseiInhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl}(1H-1,2,4-triazol-1-yl)methanone (JJKK-048).
    Aaltonen et al.
    J.Pharmacol.Exp.Ther., 2016;359:62

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