2. Metabolic Enzyme/Protease
  3. MAGL
  4. JNJ-42226314

JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.

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JNJ-42226314 Chemical Structure

JNJ-42226314 Chemical Structure

CAS No. : 1252765-13-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

JNJ-42226314 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain[1].

In Vitro

JNJ-42226314 has IC50s of 1.13 nM, 1.88 nM, 0.67 nM, 0.97 nM for human Hela cells, human PBMC, mouse brain and rat brain, respectively[1].

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

JNJ-42226314 Related Antibodies
In Vivo

JNJ-42226314 (i.p.; 3 mg/kg and 30 mg/kg; 120 min) dose-dependently elevates hippocampal 2-AG in vivo[1].
JNJ-42226314 (i.p.; 30 mg/kg)significantly increases total wake time for up to 8 hours afterward, whereas total wake time was only elevated for 2 hr following a 3 mg/kg dose[1].
JNJ-42226314 (i.p.; 30 mg/kg) is antinociceptive in the rat complete Freund’s adjuvant (CFA) model of inflammatory pain[1].
JNJ-42226314 has t1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively[1].

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

Animal Model: Male C57Bl/6 mice weighing 20-30g and male Sprague-Dawley rats weighing 300-400 g[1]
Dosage: 3 mg/kg and 30 mg/kg
Administration: i.p.; 120 min
Result: Dose-dependently elevated hippocampal 2-AG in vivo.
Molecular Weight

489.56

Formula

C26H24FN5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C2CN(C(C3=CC4=C(N(C5=CC=C(F)C=C5)C=C4)C=C3)=O)C2)CC1)C6=NC=CS6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (510.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0427 mL 10.2133 mL 20.4265 mL
5 mM 0.4085 mL 2.0427 mL 4.0853 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 6.25 mg/mL (12.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 6.25 mg/mL (12.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0427 mL 10.2133 mL 20.4265 mL 51.0663 mL
5 mM 0.4085 mL 2.0427 mL 4.0853 mL 10.2133 mL
10 mM 0.2043 mL 1.0213 mL 2.0427 mL 5.1066 mL
15 mM 0.1362 mL 0.6809 mL 1.3618 mL 3.4044 mL
20 mM 0.1021 mL 0.5107 mL 1.0213 mL 2.5533 mL
25 mM 0.0817 mL 0.4085 mL 0.8171 mL 2.0427 mL
30 mM 0.0681 mL 0.3404 mL 0.6809 mL 1.7022 mL
40 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
50 mM 0.0409 mL 0.2043 mL 0.4085 mL 1.0213 mL
60 mM 0.0340 mL 0.1702 mL 0.3404 mL 0.8511 mL
80 mM 0.0255 mL 0.1277 mL 0.2553 mL 0.6383 mL
100 mM 0.0204 mL 0.1021 mL 0.2043 mL 0.5107 mL
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JNJ-42226314 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-422263141252765-13-1JNJ42226314JNJ 42226314MAGLMonoacylglycerol lipasecompetitivereversiblenon-covalent2-arachidonoylglycerol2-AGneuropathicinflammatorypainInhibitorinhibitorinhibit

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