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252977-51-8

中文名称 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
CAS 252977-51-8
分子式 C20H22FN7O
分子量 395.43
MOL 文件 252977-51-8.mol
更新日期 2023/03/20 15:41:21
252977-51-8 结构式 252977-51-8 结构式

基本信息

中文别名
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
英文别名
TPA 023
7-tert-butyl-6-[(2-ethyl-1,2,4-triazol-3-yl)methoxy]-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine
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
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)-

物理化学性质

密度1.33±0.1 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度Soluble in DMSO
酸度系数(pKa)2.08±0.10(Predicted)
形态Solid
颜色White to off-white

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS07
警示词警告
危险性描述H302-H315-H319-H335

图谱信息

TPA 023价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-101640TPA 023
TPA 023
252977-51-81mg830元
2025/05/22HY-101640TPA 023
TPA 023
252977-51-85mg1661元
2025/05/22HY-101640TPA 023
TPA 023
252977-51-810mg2492元

常见问题列表

生物活性
TPA 023 是 GABAA α2/α3 的选择性的激动剂,Ki 值为 0.19-0.41 nM。
靶点

Ki: 0.19-0.41 nM (GABAA)

体内研究

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.

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