KML 29

Highly potent and selective MAGL inhibitor CAS# 1380424-42-9

KML 29

Catalog No. BCC6312----Order now to get a substantial discount!

Product Name & Size Price Stock
KML 29: 5mg $92 In Stock
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Quality Control of KML 29

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Chemical structure

KML 29

3D structure

Chemical Properties of KML 29

Cas No. 1380424-42-9 SDF Download SDF
PubChem ID 71656212 Appearance Powder
Formula C24H21F6NO7 M.Wt 549.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (91.01 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 1,1,1,3,3,3-hexafluoropropan-2-yl 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate
SMILES C1CN(CCC1C(C2=CC3=C(C=C2)OCO3)(C4=CC5=C(C=C4)OCO5)O)C(=O)OC(C(F)(F)F)C(F)(F)F
Standard InChIKey SXHQLPHDBLTFPM-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H21F6NO7/c25-23(26,27)20(24(28,29)30)38-21(32)31-7-5-13(6-8-31)22(33,14-1-3-16-18(9-14)36-11-34-16)15-2-4-17-19(10-15)37-12-35-17/h1-4,9-10,13,20,33H,5-8,11-12H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of KML 29

DescriptionHighly selective and potent monoacylglycerol lipase (MAGL) inhibitor. Exhibits potent inhibition of human, mouse and rat MAGL (IC50 values are 5.9, 15 and 43 nM, respectively). Exhibits no detectable inhibition of FAAH (IC50 > 50000 nM). Potently and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50 = 2.5 nM and >50 μM for 2-AG and AEA respectively).

KML 29 Dilution Calculator

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KML 29 Molarity Calculator

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Preparing Stock Solutions of KML 29

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8201 mL 9.1005 mL 18.201 mL 36.402 mL 45.5025 mL
5 mM 0.364 mL 1.8201 mL 3.6402 mL 7.2804 mL 9.1005 mL
10 mM 0.182 mL 0.9101 mL 1.8201 mL 3.6402 mL 4.5503 mL
50 mM 0.0364 mL 0.182 mL 0.364 mL 0.728 mL 0.9101 mL
100 mM 0.0182 mL 0.091 mL 0.182 mL 0.364 mL 0.455 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
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Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on KML 29

KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively. IC50 value: 15, 43, and 5.9 nM (mouse, rat, and human brain proteomes) Target: MAGL in vitro: KML29 potently and selectively inhibits MAGL with minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.[1] in vivo: KML29 a potentially very useful tool to explore the consequences of inhibiting MAGL in the whole animal and in multiple species, and provides greater selectivity than JZL184 in inhibiting MAGL. [2]

References:
[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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References on KML 29

Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates.[Pubmed:22542104]

Chem Biol. 2012 May 25;19(5):579-88.

The endocannabinoids 2-arachidonoyl glycerol (2-AG) and N-arachidonoyl ethanolamine (anandamide) are principally degraded by monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. The recent discovery of O-aryl carbamates such as JZL184 as selective MAGL inhibitors has enabled functional investigation of 2-AG signaling pathways in vivo. Nonetheless, JZL184 and other reported MAGL inhibitors still display low-level cross-reactivity with FAAH and peripheral carboxylesterases, which can complicate their use in certain biological studies. Here, we report a distinct class of O-hexafluoroisopropyl (HFIP) carbamates that inhibits MAGL in vitro and in vivo with excellent potency and greatly improved selectivity, including showing no detectable cross-reactivity with FAAH. These findings designate HFIP carbamates as a versatile chemotype for inhibiting MAGL and should encourage the pursuit of other serine hydrolase inhibitors that bear reactive groups resembling the structures of natural substrates.

Description

KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.

Keywords:

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