JZP-361( —— )

Catalog No. M34301 CAS No. 1680193-80-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

JZP-361
Note

Research use only, not for human use.
Brief Description

JZP-361 is a specific MAGL inhibitor with IC50s of 46 nM, 7.24 μM, and 1.79 μM for human recombinant MAGL, human recombinant FAAH, and human hABHD6.
Description

JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.
In Vitro

JZP-361 has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50 = 7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50 = 1.79 μM).JZP-361 retains H1 antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM.JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole.
In Vivo

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Synonyms

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Pathway

Metabolic Enzyme/Protease
Target

Lipase
Recptor

Lipase
Research Area

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Indication

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1. Jayendra Z Patel,?et al. Loratadine analogues as MAGL inhibitors. Bioorg Med Chem Lett.?2015 Apr 1;25(7):1436-42.?

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