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Submit ReviewKML 29 is a 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).
Sold under license from The Scripps Research Institute
KML 29 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 54.94 | 100 |
The following data is based on the product molecular weight 549.42. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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
If you know of a relevant reference for KML 29, please let us know.
Keywords: KML 29, KML 29 supplier, KML29, MAGL, inhibitor, MAG, lipase, monoacylglycerol, inhibitors, MGL, endocannabinoids, 2, AG, arachidonoylethanolamide, anandamide, inhibits, 4872, Tocris Bioscience
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
Margaret M et al (2019) Microglial Phagocytosis of Newborn Cells Is Induced by Endocannabinoids and Sculpts Sex Differences in Juvenile Rat Social Play. Neuron 102 435-449.e6 PMID: 30827729
Do you know of a great paper that uses KML 29 from Tocris? Please let us know.
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