产品说明
应用
JZL 184 hydrate has been used as an inhibitor of monoacylglycerol lipase to study its effect on human osteoblast differentiation and proliferation and postsynaptic neurons.
包装
5 mg in glass bottle
生化/生理作用
JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.
特点和优势
This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
基本信息
| 经验(实验)分子式 | C27H24N2O9 · xH2O |
| 分子量 | 520.49 (anhydrous basis) |
| MDL编号 | MFCD12912421 |
| PubChem化学物质编号 | 329815406 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | powder |
| 颜色 | light yellow to yellow-green |
| 溶解性 | DMSO: >20 mg/mL |
| 储存温度 | 2-8℃ |
| SMILES string | O.OC(C1CCN(CC1)C(=O)Oc2ccc(cc2)[N+]([O-])=O)(c3ccc4OCOc4c3)c5ccc6OCOc6c5 |
| InChI | 1S/C27H24N2O9.H2O/c30-26(38-21-5-3-20(4-6-21)29(32)33)28-11-9-17(10-12-28)27(31,18-1-7-22-24(13-18)36-15-34-22)19-2-8-23-25(14-19)37-16-35-23;/h1-8,13-14,17,31H,9-12,15-16H2;1H2 |
| InChI key | HNSBVGMOKGQJLT-UHFFFAOYSA-N |
安全信息
| 象形图 |  |
| 警示用语： | Danger |
| 危险声明 | H301 |
| 预防措施声明 | P301 + P310 |
| 危险分类 | Acute Tox. 3 Oral |
| 储存分类代码 | 6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
