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

475741
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Přehled

Replacement Information

Tabulka spec. kláve

CAS #Empirical Formula
1101854-58-3C₂₇H₂₄N₂O₉

Products

Katalogové čísloBalení ks/bal.
475741-10MG Skleněná láhev 10 mg
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
Katalogové číslo GTIN
475741-10MG 04055977185577

Documentation

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

Title

Safety Data Sheet (SDS) 

MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem Certificates of Analysis

TitleLot Number
475741

References

Přehled odkazů
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.

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.