Cravatt Reagent 是选择性的、口服具有活性的单酰基甘油脂肪酶 (MAGL) 抑制剂,对 hMAGL 和 2-花生四烯酸甘油酯 (2-AG) 的IC50分别为 9.1 nM 和 2.1 nM。它具有阿片类药物保护作用,具有显著的抗痛觉过敏活性。
产品描述
Cravatt Reagent is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.
体内活性
The Selective Monoacylglycerol Lipase Inhibitor Cravatt Reagent Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.
动物实验
For repeated administration experiments, mice were given vehicle, 0.0818 mg/kg MJN110, 0.469 or 10 mg/kg morphine, or a combination of 0.0818 mg/kg Cravatt Reagent?and 0.469 mg/kg morphine twice?daily for 5.5 days.?Then, mice underwent behavioral testing on day 6.?The combination of 0.0818 mg/kg MJN110 and 0.469 mg/kg morphine produced significant antinociceptive effects.
Cas No.
1438416-21-7
分子式
C22H21Cl2N3O4
分子量
462.33
别名
Cravatt Reagent
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years