半岛bd体育手机客户端 说明
一般描述
A cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, bothin vitro(IC50= 6 - 8 nM against 2-AG hydrolysis by MAGL vs. 4 ?M against anandamide/AEA hydrolysis by FAAH) and in micein vivo(5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling andin vivophysiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
A cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, bothin vitro(IC50= 6-8 nM against 2-AG hydrolysis by MAGL vs. 4 ?M against anandamide/AEA hydrolysis by FAAH) and in micein vivo(5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling andin vivophysiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
包装
10 mg in Glass bottle
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Nomura, D.K., et al. 2010.Cell140,49.
Long, J.Z., et al.Nature Chem. Biol.16,744.
Long, J.Z., et al. 2009.Nature Chem. Biol.5,37.
Pan, B., et al. 2009.J. Pharmacol. Exp. Ther.331,591.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C27H24N2O9 |
| 分子量 | 520.49 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white to off-white |
| 溶解性 | DMSO: 50 mg/mL |
| 运输 | wet ice |
| 储存温度 | ?20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
