5.33088

Monoacylglycerol Lipase Inhibitor, Cpd21

• 别名: Monoacylglycerol Lipase Inhibitor, Cpd21, MAGL Inhibitor, Cpd21
• 经验公式（希尔记法）: C₂₆H₂₆O₄
• CAS号: 1643657-35-5
• 分子量: 402.48
• UNSPSC代码: 12352200

属性

• 方案: ≥98% (HPLC)
• 质量水平: 100
• 表单: solid
• 效能: 400 nM K_i
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: off-white
• 溶解性: DMSO: 50 mg/mL
• 储存温度: 2-8°C

说明

一般描述

A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, K_i = 400 nM, IC₅₀ = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC₅₀ = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC₅₀ = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.

MAGL inhibitor, Monoacylglycerol Lipase Inhibitor

生化/生理作用

Cell permeable: yes

Primary Target
MAGL

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

Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable