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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M651194-5mg |
5mg |
期货 ![]() |
| |
| M651194-10mg |
10mg |
期货 ![]() |
|
| 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% |
| 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= |
| 溶解性 | DMSO : 100 mg/mL (274.11 mM; Need ultrasonic) |
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