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MAGL-IN-4
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MAGL-IN-4图片
CAS NO:2135785-20-3
包装与价格：
包装价格(元)
5mg询价
10mg询价

MAGL-IN-4 是一种口服有效，选择性和可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂，IC50 为 6.2 nM。MAGL-IN-4 可以穿透血脑屏障 (BBB)。MAGL-IN-4 主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油 (2-AG) 水平来增强内源性大麻素信号。
Cas No.2135785-20-3
分子式C18H21ClN2O4
分子量364.82
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1].

MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1]. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1].

MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1].

[1]. Shuhei Ikeda, et al. Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044.

 
 
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