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MAGL-IN-4

    级别和纯度:
  • ≥99%
  • CAS编号: 2135785-20-3
  • 分子式: C18H21ClN2O4
  • 分子量: 364.82
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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
M651194-5mg
5mg 期货 Stock Image
M651194-10mg
10mg 期货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 MAGL-IN-4
生化机理 MAGL-IN-4 是一种口服活性、选择性和可逆性单酰基甘油脂肪酶(MAGL)抑制剂,其 IC 50 为 6.2 nM。MAGL-IN-4 可穿透血脑屏障(BBB)。MAGL-IN-4 能增强内源性大麻素信号转导,主要是通过增加内源性大麻素的浓度来实现的。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC 50 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.

In Vitro

MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC 50 >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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

纯度 ≥99%

名称和识别符

分子量 364.82
Reaxy-Rn 31787717
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31787717&ln=

化学和物理性质

溶解性 DMSO : 100 mg/mL (274.11 mM; Need ultrasonic)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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