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Submit ReviewJJKK 048
说明： Potent and selective MAGL inhibitor
化学名： 4-[Bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl]-1H-1,2,4-triazol-1-yl-methanone
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for JJKK 048
JJKK 048 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for JJKK 048
| 分子量 | 434.44 |
| 公式 | C23H22N4O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for JJKK 048
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 43.44 | 100 |
制备储备液 for JJKK 048
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for JJKK 048
参考文献 for JJKK 048
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for JJKK 048, please let us know.
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关键词: JJKK 048, JJKK 048 supplier, JJKK048, potent, selective, MAGL, inhibitors, inhibits, monoacylglycerol, lipases, hydrolases, analgesic, analgesia, 5206, Tocris Bioscience
1 篇 JJKK 048 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JJKK 048 的部分引用包括：
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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