化合物TTA-A2 T8944

Product Introduction
Bioactivity


英文名: TTA-A2

描述: TTA-A2 是一种选择性 T 型钙通道拮抗剂，是一种有效的抗惊厥药，可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。

体内活性: TTA-A2 (oral gavage; 10 mg/kg; once daily; 5 days) shows selective effect on recurrent thalamocortical network activity, it suppresses active wake and promotes slow-wave sleep in wild-type mice but not in mice lacking both Cav3.1 and Cav3.3[1].TTA-A2 (oral gavage;?3 mg/kg;?single dose) produces significant changes in sleep architecture in rats.?A reduction in active wake soon after dosing with a concurrent increase in delta sleep and decrease in REM sleep.?Additionally, these effects persists for up to 4 h post-dose in rats[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 27.5 mg/mL (72.68 mM)


关键字: Pregnane X receptor | neurological diseases | T-type calcium channel | Inhibitor | Ca2+ channels | Ca channels | Electrocorticogram | TTAA2 | sleep disorders | TTA-A2 | TTA-A-2 | inhibit | TTA A2 | Epilepsy | Calcium Channel

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途