| 规格或纯度 | ≥98%(HPLC) |
|---|---|
| 英文名称 | JJKK 048 |
| 别名 | 4-[双(1,3-苯并二恶唑-5-基)甲基] -1-哌啶基] -1H-1,2,4-三唑-1-基-甲酮 |
| 生化机理 | 有效的选择性单酰基甘油脂肪酶（MAGL）抑制剂（IC50 = 0.4 nM）。相对于FAAH和ABHD6，MAGL的选择性分别> 13,000和?630倍。增加体内小鼠体内2-花生四烯酰甘油（2-AG）水平的水平。促进疼痛模型中的镇痛作用。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| IUPAC Name | [4-[bis(1,3-benzodioxol-5-yl)methyl]piperidin-1-yl]-(1,2,4-triazol-1-yl)methanone |
|---|---|
| INCHI | InChI=1S/C23H22N4O5/c28-23(27-12-24-11-25-27)26-7-5-15(6-8-26)22(16-1-3-18-20(9-16)31-13-29-18)17-2-4-19-21(10-17)32-14-30-19/h1-4,9-12,15,22H,5-8,13-14H2 |
| InChi Key | CLSNATLUIXZPMV-UHFFFAOYSA-N |
| Canonical SMILES | C1CN(CCC1C(C2=CC3=C(C=C2)OCO3)C4=CC5=C(C=C4)OCO5)C(=O)N6C=NC=N6 |
| PubChem CID | 76313567 |
| 分子量 | 434.44 |
| 溶解性 | 溶于DMSO, 最高浓度 (mg/mL): 43.44, 最高浓度(mM): 100 |
|---|
| RIDADR | NONHforallmodesoftransport |
|---|
| Ligand ID | 9481 |
|---|---|
| 名称 | JJKK 048 |
| 别名 | JJKK-048 |
| 类别 | Synthetic organic |
| 学名 | [4-[bis(1,3-benzodioxol-5-yl)methyl]piperidin-1-yl]-(1,2,4-triazol-1-yl)methanone |
| 生物活性评价 |
The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in |
| 评价 |
Potent and selective monoacylglycerol lipase (MAGL) inhibitor |
| 1. Aaltonen N, Savinainen JR, Ribas CR, R?nkk? J, Kuusisto A, Korhonen J, Navia-Paldanius D, H?yrinen J, Takabe P, K?sn?nen H et al.. (2013) Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase.. Chem Biol, 20 (3): (379-90). [PMID:23521796] |
| 2. Aaltonen N, Kedzierska E, Orzelska-Górka J, Lehtonen M, Navia-Paldanius D, Jakupovic H, Savinainen JR, Nevalainen T, Laitinen JT, Parkkari T et al.. (2016) In Vivo Characterization of the Ultrapotent Monoacylglycerol Lipase Inhibitor {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 (1): (62-72). [PMID:27451409] |
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