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475741 MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem

The MAGL Inhibitor III, JZL184, also referenced under CAS 1101854-58-3, controls the biological activity of MAGL.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184

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475741
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Tableau de caractéristiques principal

CAS #Empirical Formula
1101854-58-3C₂₇H₂₄N₂O₉

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      Description
      OverviewA cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, both in vitro (IC50 = 6 - 8 nM against 2-AG hydrolysis by MAGL vs. 4 µM against anandamide/AEA hydrolysis by FAAH) and in mice in vivo (5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling and in vivo physiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
      Catalogue Number475741
      Brand Family Calbiochem®
      Synonyms4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184
      References
      ReferencesNomura, D.K., et al. 2010. Cell 140, 49.
      Long, J.Z., et al. Nature Chem. Biol. 16, 744.
      Long, J.Z., et al. 2009. Nature Chem. Biol. 5, 37.
      Pan, B., et al. 2009. J. Pharmacol. Exp. Ther. 331, 591.
      Product Information
      CAS number1101854-58-3
      FormWhite to off-white solid
      Hill FormulaC₂₇H₂₄N₂O₉
      Chemical formulaC₂₇H₂₄N₂O₉
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      475741-10MG 04055977185577

      Documentation

      MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      475741

      Références bibliographiques

      Aperçu de la référence bibliographique
      Nomura, D.K., et al. 2010. Cell 140, 49.
      Long, J.Z., et al. Nature Chem. Biol. 16, 744.
      Long, J.Z., et al. 2009. Nature Chem. Biol. 5, 37.
      Pan, B., et al. 2009. J. Pharmacol. Exp. Ther. 331, 591.
      Fiche technique

      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.

      Revision17-December-2018 JSW
      Synonyms4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184
      DescriptionA cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, both in vitro (IC50 = 6-8 nM against 2-AG hydrolysis by MAGL vs. 4 µM against anandamide/AEA hydrolysis by FAAH) and in mice in vivo (5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling and in vivo physiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
      FormWhite to off-white solid
      CAS number1101854-58-3
      Chemical formulaC₂₇H₂₄N₂O₉
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°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
      ReferencesNomura, D.K., et al. 2010. Cell 140, 49.
      Long, J.Z., et al. Nature Chem. Biol. 16, 744.
      Long, J.Z., et al. 2009. Nature Chem. Biol. 5, 37.
      Pan, B., et al. 2009. J. Pharmacol. Exp. Ther. 331, 591.