| 货号 | 3817/50 |
| 别名 | 3-(1,1-Dimethylethyl)-7-(5-methyl-3 |
| 供应商 | Tocris |
| 生物活性 | GABAA receptor inverse agonist selective for the α5-subtype (EC50 = 3 nM). Exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-,α1-,α2-, and α5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 368.39 |
| 分子式 | C17H20N8O2 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 10 mM in ethanol |
| CAS号 | 783331-24-8 |
| 参考文献 | Atacket al (2009) In vitro and in vivo properties of 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 (MRK-016), a GABAA receptor α5 subtype-selective inverse agonist. J.Pharmacol.Exp.Ther. 331 470. PMID: 19704033. Chamberset al (2004) An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA α5 receptors with cognition enhancing properties. J.Med.Chem. 47 5829. PMID: 15537339. |