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MAGL-IN-4 (His121 ARG57) 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂,IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。
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MAGL-IN-4 (His121 ARG57) 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂,IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,450 | 现货 | |
5 mg | ¥ 3,480 | 现货 | |
10 mg | ¥ 4,850 | 现货 | |
25 mg | ¥ 7,750 | 现货 | |
50 mg | ¥ 9,870 | 现货 | |
100 mg | ¥ 13,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,830 | 现货 |
产品描述 | MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases. |
靶点活性 | MAGL:6.2 nM |
体外活性 | MAGL-IN-4 showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption and blood-brain barrier penetration[1]. |
体内活性 | MAGL-IN-4 showed significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice[1]. |
别名 | His121 ARG57 |
分子量 | 364.82 |
分子式 | C18H21ClN2O4 |
CAS No. | 2135785-20-3 |
Smiles | Cc1ccc(COC2CN(C2)C(=O)[C@H]2C[C@@]3(C2)COC(=O)N3)cc1Cl |
密度 | 1.38 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 88 mg/mL (241.21 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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