JJKK 048

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Cat.No. 5206 - JJKK 048 | C23H22N4O5 | CAS No. 1515855-97-6
Description: Potent and selective MAGL inhibitor
Chemical Name: 4-[Bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl]-1H-1,2,4-triazol-1-yl-methanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective monoacylglycerol lipase (MAGL) inhibitor (IC50 = 0.4 nM). Exhibits >13,000 and ~630-fold selectivity for MAGL over FAAH and ABHD6, respectively. Increases brain levels of 2-arachidonoylglycerol (2-AG) levels in mice in vivo. Promotes analgesia in pain models.

Technical Data

M. Wt 434.44
Formula C23H22N4O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1515855-97-6
PubChem ID 76313567
InChI Key CLSNATLUIXZPMV-UHFFFAOYSA-N
Smiles O=C(N6C=NC=N6)N(CC5)CCC5C(C2=CC=C(OCO3)C3=C2)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 43.44 100

Preparing Stock Solutions

The following data is based on the product molecular weight 434.44. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.3 mL 11.51 mL 23.02 mL
5 mM 0.46 mL 2.3 mL 4.6 mL
10 mM 0.23 mL 1.15 mL 2.3 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Aaltonen et al (2013) Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem.Biol. 20 379 PMID: 23521796

Laitinen et al (2014) Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency. Mol.Pharmacol. 85 510 PMID: 24368842

Aaltonen et al (2016) In vivo characterization of the ultrapotent monoacylglycerol lipaseiInhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl}(1H-1,2,4-triazol-1-yl)methanone (JJKK-048). J.Pharmacol.Exp.Ther. 359 62 PMID: 27451409


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