2. Metabolic Enzyme/Protease
  3. MAGL
  4. JJKK 048

JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC50 values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain.

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

JJKK 048 Chemical Structure

JJKK 048 Chemical Structure

CAS No. : 1515855-97-6

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

JJKK 048 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE JJKK 048

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC50 values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain[1][2].

IC50 & Target

MAGL[1]
Cellular Effect
Cell Line Type Value Description References
COS-7 IC50
4800 nM
Compound: JJKK-048
Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
[PMID: 25282655]
HEK293 IC50
0.4 nM
Compound: JJKK-048
Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
[PMID: 25282655]
In Vitro

JJKK 048 covalently binds to the serine (S122) at the active site of MAGL to form a carbamate adduct, inhibiting the hydrolysis of 2-Arachidonoylglycerol (HY-W011051) (2-AG) by MAGL and thus increasing the tissue levels of 2-AG[1][2].
JJKK 048 selectively increases tissue levels of 2-AG but not AEA of endocannabinoid levels in inhibitor-treated brain sections[1].
JJKK 048 inhibits 2-AG hydrolysis in a dose-dependent manner in intact HEK293 cells transiently overexpressing human MAGL[1].

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

JJKK 048 Related Antibodies
In Vivo

JJKK 048 (0.1-4 mg/kg; i.p.; single dose; acute administration) potently inhibits MAGL and elevates brain 2-Arachidonoylglycerol (2-AG) (HY-W011051) levels in male C57Bl/6J mice[2].
JJKK 048 (0.5-2 mg/kg; i.p.; single dose; acute administration) inhibits MAGL in peripheral tissues (liver, spleen, heart, and skeletal muscle) with some off - target effects in mouse[2].
JJKK 048 (0.5 mg/kg; i.p.; single dose; acute administration) promotes significant analgesia in a writhing test in male Albino Swiss mice without causing cannabimimetic side effects[2].
JJKK 048 (1-2 mg/kg; i.p.; single dose; acute administration) induces analgesia both in the writhing test and in the tail - immersion test, as well as hypomotility and hyperthermia, but not catalepsy in male Albino Swiss mice[2].

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

Animal Model: Male C57Bl/6J mice (8 weeks old, weight 20-26 g)[2]
Dosage: 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, (dissolved in 5% (v/v) dimethylsulfoxide (DMSO) in gently heated 10% (w/v) HP-β-CD (HY-101103))
Administration: i.p., single dose
Result: Revealed a dose-dependent blockade of MAGL in the brain.
Increased brain 2-AG levels in a dose-dependent manner, while brain AEA levels remained unaffected.
Animal Model: Male Albino Swiss mice (weight 20-30 g), tetrad test model for cannabimimetic effects[2]
Dosage: 0.5 mg/kg, 1 mg/kg, 2 mg/kg (dissolved in 5% (v/v) DMSO in gently heated 10% (w/v) HP-β-CD (HY-101103))
Administration: i.p., single dose
Result: Caused significant reduction in the writhing episodes of mice in the writhing test, indicating an antinociceptive effect.
Molecular Weight

434.44

Formula

C23H22N4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC(C(C2=CC=C(OCO3)C3=C2)C4=CC=C(OCO5)C5=C4)CC1)N6N=CN=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (76.72 mM; ultrasonic and warming and heat to 60°C; 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 2.3018 mL 11.5091 mL 23.0181 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

Purity: 99.55%

SDS (393 KB)

COA (257 KB) RP-HPLC (208 KB) MS (181 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3018 mL 11.5091 mL 23.0181 mL 57.5453 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 mL 11.5091 mL
10 mM 0.2302 mL 1.1509 mL 2.3018 mL 5.7545 mL
15 mM 0.1535 mL 0.7673 mL 1.5345 mL 3.8364 mL
20 mM 0.1151 mL 0.5755 mL 1.1509 mL 2.8773 mL
25 mM 0.0921 mL 0.4604 mL 0.9207 mL 2.3018 mL
30 mM 0.0767 mL 0.3836 mL 0.7673 mL 1.9182 mL
40 mM 0.0575 mL 0.2877 mL 0.5755 mL 1.4386 mL
50 mM 0.0460 mL 0.2302 mL 0.4604 mL 1.1509 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9591 mL
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JJKK 048 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:

JJKK 0481515855-97-6JJKK048JJKK-048MAGLMonoacylglycerol lipaseInhibitorinhibitorinhibit

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