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533088 Monoacylglycerol Lipase Inhibitor, Cpd21 - Calbiochem

533088
  
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      Overview

      Replacement Information

      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
      Applications
      Biological Information
      Primary TargetMAGL
      Primary Target K<sub>i</sub>400 nM, IC₅₀
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      533088 0

      Documentation

      Monoacylglycerol Lipase Inhibitor, Cpd21 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl. 53, in press.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision01-March-2016 JSW
      SynonymsMAGL Inhibitor, Cpd21
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₆H₂₆O₄
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesHernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl. 53, in press.