JZL184

Catalog No.S4904

For research use only.

JZL 184 is the first selective inhibitor of monoacylglycerol lipase (MAGL) with IC50 of 8 nM.

JZL184 Chemical Structure

CAS No. 1101854-58-3

Selleck's JZL184 has been cited by 7 Publications

Purity & Quality Control

Choose Selective Lipase Inhibitors

Biological Activity

Description JZL 184 is the first selective inhibitor of monoacylglycerol lipase (MAGL) with IC50 of 8 nM.
Targets
MAGL [1]
8 nM
In vitro

JZL184 is a useful tool for studying the effects of endogenous 2-AG signaling. JZL184 displays time-dependent inhibition of MAGL and exhibits >300-fold selectivity for MAGL over FAAH in vitro. JZL184 does not interact with CB1 or CB2 receptors and does not inhibit the 2-AG biosynthetic enzymes diacylglycerol lipase-αand diacylglycerol lipase-β, or the arachidonic acid–mobilizing enzyme cytosolic phospholipase A2 group IVA. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 cells MYLGeY5kfGmxbjDhd5NigQ>? M3jseGlvcGmkaYTpc44hd2ZiaIXtZY4hVUGJTDDlfJBz\XO|ZXSgbY4hdW:wa3X5JGNQWzdiY3XscJMtKEmFNUC9NE4xODJizszN MonYNlM1PTVyNUi=
COS7 cells M17XPGZ2dmO2aX;uJIF{e2G7 NVHCZYJmUW6qaXLpeIlwdiCxZjDoeY1idiCPQVfMJIV5eHKnc4Pl[EBqdiCFT2O3JINmdGy|IIXzbY5oKGWwZH;n[Y5wfXNiMj3BS{B{fWK|dILheIUtKEmFNUC9NE4xODJizszN NF7pWngzOjd|OE[zPC=>
In vivo JZL184 produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in eight-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL184-treated mice showed a wide array of CB1-dependent behavioral effects, including analgesia, hypomotility and hypothermia, that suggest a broad role for 2-AG–mediated endocannabinoid signaling throughout the mammalian nervous system. [1]

Protocol (from reference)

Kinase Assay:[1]
  • activity-based protein profiling (ABPP):

    Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s

Cell Research:[2]
  • Cell lines: LOVO, Caco-2, SW480
  • Concentrations: 0.5 μg/μL
  • Incubation Time: 24 h
  • Method: 1 × 105 cells are split into four-well chamber slides and incubated with culture medium containing BrdU for 4 h. BrdU staining is performed following the manufacturer’s instructions.
Animal Research:[1]
  • Animal Models: male C57Bl/6 mice
  • Dosages: 4-40 mg/kg
  • Administration: Intraperitoneally or oral gavage

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+ddH2O
For best results, use promptly after mixing.

2.5mg/ml

Chemical Information

Molecular Weight 520.49
Formula

C27H24N2O9

CAS No. 1101854-58-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1C(C2=CC3=C(C=C2)OCO3)(C4=CC5=C(C=C4)OCO5)O)C(=O)OC6=CC=C(C=C6)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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