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

KML29 

Cat. No.: HY-18977 Purity: 98.87%
Handling Instructions

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.

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

KML29 Chemical Structure

KML29 Chemical Structure

CAS No. : 1380424-42-9

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 73 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
Estimated Time of Arrival: December 31
100 mg USD 696 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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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].

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

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].

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.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (91.01 mM; Need ultrasonic)

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
10 mM 0.1820 mL 0.9101 mL 1.8201 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 (4.55 mM); Clear solution

  • 2.

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

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

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

KML29KML 29KML-29MAGLMonoacylglycerol lipaseallodyniaHFIP2-AGLPSInhibitorinhibitorinhibit

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Product Name:
KML29
Cat. No.:
HY-18977
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