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533088 Monoacylglycerol Lipase Inhibitor, Cpd21 - Calbiochem

533088
  
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      Overview

      Key Spec Table

      Empirical Formula
      C₂₆H₂₆O₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, Ki = 400 nM, IC50 = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC50 = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC50 = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.

      Catalogue Number533088
      Brand Family Calbiochem®
      SynonymsMAGL Inhibitor, Cpd21
      References
      ReferencesHernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl. 53, in press.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₆H₂₆O₄
      Chemical formulaC₂₆H₂₆O₄
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetMAGL
      Primary Target K<sub>i</sub>400 nM, IC₅₀
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      533088 0