TPA 023
| 中文名称 | TPA 023 |
|---|---|
| 中文同义词 | 7-(叔丁基)-6-((1-乙基-1H-1,2,4-三唑-5-基)甲氧基)-3-(2-氟苯基)-[1,2,4]三唑并[4,3-B]哒嗪;化合物 T17144;化合物TPA 023 |
| 英文名称 | 7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine |
| 英文同义词 | TPA 023;7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine;7-tert-butyl-6-[(2-ethyl-1,2,4-triazol-3-yl)methoxy]-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine;1,2,4-Triazolo[4,3-b]pyridazine, 7-(1,1-dimethylethyl)-6-[(1-ethyl-1H-1,2,4-triazol-5-yl)methoxy]-3-(2-fluorophenyl)-;inhibit,γ-Aminobutyric acid Receptor,TPA 023,Inhibitor,Gamma-aminobutyric acid Receptor,TPA-023,GABA Receptor,TPA023 |
| CAS号 | 252977-51-8 |
| 分子式 | C20H22FN7O |
| 分子量 | 395.43 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 252977-51-8.mol |
| 结构式 |  |
TPA 023 性质
| 密度 | 1.33±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 2.08±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
Ki: 0.19-0.41 nM (GABAA)
TPA023 displays good receptor occupancy, when administered orally to rats. The dose of TPA023 resulting in 50% occupancy of rat brain GABAA receptors is 0.42 mg/kg, with the corresponding plasma concentration being 25 ng/mL. TPA023 is also efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection at a dose of 10 mg/kg i.p. (84% occupancy), with the ED 50 of 0.19-0.41 nM, for protection against tonic convulsions (1.4 mg/kg i.p.) corresponding to around 50% occupancy. TPA023 (3 mg/kg p.o. in 0.5% methyl cellulose) shows anxiolytic-like effect on rats. TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101640 | TPA 023 TPA 023 | 252977-51-8 | 1mg | 4500元 |
| 2024/04/30 | HY-101640 | TPA 023 TPA 023 | 252977-51-8 | 5mg | 8900元 |