KML 29

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Cat.No. 4872 - KML 29 | C24H21F6NO7 | CAS No. 1380424-42-9
Description: Highly potent and selective MAGL inhibitor
Chemical Name: 4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Highly 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).

Licensing Information

Sold under license from The Scripps Research Institute

Technical Data

M. Wt 549.42
Formula C24H21F6NO7
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1380424-42-9
PubChem ID 71656212
InChI Key SXHQLPHDBLTFPM-UHFFFAOYSA-N
Smiles O=C(OC(C(F)(F)F)C(F)(F)F)N(CC5)CCC5C(C2=CC=C(OCO3)C3=C2)(O)C1=CC(OCO4)=C4C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 549.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.82 mL 9.1 mL 18.2 mL
5 mM 0.36 mL 1.82 mL 3.64 mL
10 mM 0.18 mL 0.91 mL 1.82 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Ueda et al (2012) Discrimination between two endocannabinoids. Chem.Biol. 19 545 PMID: 22633404

Chang et al (2012) Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem.Biol. 19 579 PMID: 22542104


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Keywords: KML 29, KML 29 supplier, KML29, MAGL, inhibitor, MAG, lipase, monoacylglycerol, inhibitors, MGL, endocannabinoids, 2, AG, arachidonoylethanolamide, anandamide, inhibits, 4872, Tocris Bioscience

1 Citation for KML 29

Citations are publications that use Tocris products. Selected citations for KML 29 include:

Morena et al (2016) Emotional arousal state influences the ability of amygdalar endocannabinoid signaling to modulate anxiety. Neuropharmacology 111 59 PMID: 27553121


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