| Bioactivity | TTA-A8 (Compound 13) is a short-acting T-type calcium channel antagonist with oral activity, exhibiting an IC50 value of 31.3 nM in the FLIPR depolarization assay. TTA-A8 possesses favorable pharmacokinetic properties, making it suitable for research on epilepsy and sleep[1]. |
| In Vivo | TTA-A8 (3 mg/kg; 口服; 单剂量) 在遗传失神性癫痫的 Wistar 白化大鼠模型中能有效减短癫痫发作时间。TTA-A8 (1-10 mg/kg; 口服; 单剂量) 在 SD 大鼠中显著抑制了 active wake，并增加了 δ 波睡眠[1]。TTA-A8 (5 mg/kg; 口服; 单剂量) 在三个临床前物种 (大鼠、犬、恒河猴) 中表现出中高的血浆清除率 (CLp)，低至低的分布体积 (Vss) 和短的半衰期 (T1/2)[1]。在大鼠、犬、恒河猴中的药代动力学分析[1]species |
| CAS | 1146395-46-1 |
| Formula | C22H21F3N4O2 |
| Molar Mass | 430.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yang Z Q, et al. Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents[J]. ACS Medicinal Chemistry Letters, 2010, 1(9): 504-509. |
TTA-A8
CAS: 1146395-46-1 F: C22H21F3N4O2 W: 430.42
TTA-A8 (Compound 13) is a short-acting T-type calcium channel antagonist with oral activity, exhibiting an IC50 value of
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