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Submit ReviewJJKK 048
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)
Biological Activity for JJKK 048
JJKK 048 is a 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.
Compound Libraries for JJKK 048
JJKK 048 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JJKK 048
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JJKK 048
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.44 | 100 |
Preparing Stock Solutions for JJKK 048
The following data is based on the product molecular weight 434.44. 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 | 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 for JJKK 048
References for JJKK 048
References are publications that support the biological activity of the product.
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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Keywords: JJKK 048, JJKK 048 supplier, JJKK048, potent, selective, MAGL, inhibitors, inhibits, monoacylglycerol, lipases, hydrolases, analgesic, analgesia, 5206, Tocris Bioscience
1 Citation for JJKK 048
Citations are publications that use Tocris products. Selected citations for JJKK 048 include:
Dandan et al (2017) Regulatory role of tumor necrosis factor receptor-associated factor 6 in breast cancer by activating the protein kinase B/glycogen synthase kinase 3β signaling pathway. Mol Med Rep 16 2269-2273 PMID: 28627683
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