1. Metabolic Enzyme/Protease
  2. MAGL
  3. JZL 184

JZL 184 

Cat. No.: HY-15249 Purity: 98.20%
Handling Instructions

JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.

For research use only. We do not sell to patients.

JZL 184 Chemical Structure

JZL 184 Chemical Structure

CAS No. : 1101854-58-3

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
10 mg USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 264 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH[1][2].

IC50 & Target

IC50: 8 nM (2-Arachidonoylglycerol (2-AG) hydrolysis)[1]

In Vitro

JZL 184 displays IC50 values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia[1].
JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57Bl/6 mice (6-8 weeks old, 20-26 g)[1]
Dosage: 4 mg/kg, 8 mg/kg, 16 mg/kg, 40 mg/kg
Administration: Intraperitoneal injection; once
Result: Produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that were maintained for at least 8 h.
Molecular Weight

520.49

Formula

C₂₇H₂₄N₂O₉

CAS No.

1101854-58-3

SMILES

OC(C1=CC=C(OCO2)C2=C1)(C3CCN(C(OC4=CC=C([N+]([O-])=O)C=C4)=O)CC3)C5=CC(OCO6)=C6C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (67.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9213 mL 9.6063 mL 19.2127 mL
5 mM 0.3843 mL 1.9213 mL 3.8425 mL
10 mM 0.1921 mL 0.9606 mL 1.9213 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.80 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

JZL 184JZL184JZL-184MAGLMonoacylglycerol lipase2-ArachidonoylglycerolhydrolysisanalgesiaantinociceptiveneuronsInhibitorinhibitorinhibit

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JZL 184
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