- 英文名称
- 3-(9-(tert-Butyl)-8-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazin-2-yl)-5-methylisoxazole
- 分子式
- C17H20N8O2
- 分子量
- 368.39
- 中文别名
- MRK-016; 化合物 T12105; 化合物 MRK-016; MRK-016; 3-tert-butyl-7-(5-methyl-1,2-oxazol-3-yl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazine; 7-(5-Methyl-1,2-oxazol-3-yl)-3-(2-methyl-2-propanyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazine; 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo(1,5-d)(1,2,4)triazine; MRK016; MRK 016; 3-[3-tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazole; Pyrazolo[1,5-d][1,2,4]triazine, 3-(1,1-dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-
- 用途
- MRK-016是一种选择性的，可口服的，可透过血脑屏障的GABAA α5 receptor拮抗剂，对GABAA α5的EC50值为3 nM，对人GABAA α1β3γ2、GABAA α2β3γ2、GABAA α3β3γ2和GABAA α5β3γ2的Ki值分别为0.83、0.85、0.77和1.4 nM
