2. Metabolic Enzyme/Protease
  3. MAGL
  4. KML29

KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.

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KML29 Chemical Structure

KML29 Chemical Structure

CAS No. : 1380424-42-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

KML29 Related Antibodies

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  • Purity & Documentation

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Description

KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH[1][2].

IC50 & Target

IC50: 15 nM (mouse MAGL), 43 nM (rat MAGL), 5.9 nM (human MAGL)[2].
In Vitro

KML29 dose-dependently elevates brain 2-AG level up to 10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide[2].
KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested[2].

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

KML29 Related Antibodies
In Vivo

KML29 enhibits antinociceptive activity without cannabimimetic side effects[3].
KML29 (20 mg/kg) has a significant but modest protective effect against LPS-induced fever[3].

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

Animal Model: C57Bl/6 mice[2].
Dosage: 1-40 mg/kg.
Administration: P.O. single dose.
Result: Selectively inhibited MAGL in mice.
Animal Model: Wistar albino male rats[2].
Dosage: 20 mg/kg (+LPS E. coli O111:B4 (250 µg/kg, sc)).
Administration: SC.
Result: Administration of KML29 simultaneously with LPS E. coli O111:B4 significantly decreased ∆T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111:B4. Administration of KML29 simultaneously with LPS E. coli O111:B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111:B4+saline administration.
Molecular Weight

549.42

Formula

C24H21F6NO7
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)O)CC1)OC(C(F)(F)F)C(F)(F)F
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 : 50 mg/mL (91.01 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 1.8201 mL 9.1005 mL 18.2010 mL
5 mM 0.3640 mL 1.8201 mL 3.6402 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)

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 (4.55 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.64%

COA (252 KB) RP-HPLC (219 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, 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 1.8201 mL 9.1005 mL 18.2010 mL 45.5025 mL
5 mM 0.3640 mL 1.8201 mL 3.6402 mL 9.1005 mL
10 mM 0.1820 mL 0.9101 mL 1.8201 mL 4.5503 mL
15 mM 0.1213 mL 0.6067 mL 1.2134 mL 3.0335 mL
20 mM 0.0910 mL 0.4550 mL 0.9101 mL 2.2751 mL
25 mM 0.0728 mL 0.3640 mL 0.7280 mL 1.8201 mL
30 mM 0.0607 mL 0.3034 mL 0.6067 mL 1.5168 mL
40 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1376 mL
50 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9101 mL
60 mM 0.0303 mL 0.1517 mL 0.3034 mL 0.7584 mL
80 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL
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KML29 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:

KML291380424-42-9KML 29KML-29MAGLMonoacylglycerol lipaseallodyniaHFIP2-AGLPSInhibitorinhibitorinhibit

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