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

475741
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₇H₂₄N₂O₉ 1101854-58-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475741-10MG
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          Glass bottle 10 mg
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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
          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
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          475741

          References

          Reference overview
          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.
          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.

          Revision27-February-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
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1101854-58-3
          Chemical formulaC₂₇H₂₄N₂O₉
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          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.
          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.