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KML29

Catalog No. T4052 CAS 1380424-42-9

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

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KML29, CAS 1380424-42-9

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).
Targets&IC50	human MAGL:5.9 nM, rat MAGL:43 nM, AEA:>50 μM, 2-AG:2.5 nM, mouse MAGL:15 nM
In vivo	DprE1-IN-2 has efficacy in a rodent model of tuberculosis.

Molecular Weight	549.42
Formula	C24H21F6NO7
CAS No.	1380424-42-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (91 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Chang JW, et al. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem Biol. 2012 May 25;19(5):579-588. 2. Ignatowska-Jankowska BM,et al. In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects. Br J Pharmacol. 2014 Mar;171(6):1392-1407.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KML29 1380424-42-9 Metabolism Lipase LPS allodynia Monoacylglycerol lipase MAGL inhibit 2-AG Inhibitor HFIP KML 29 KML-29 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.