ACT-709478是一种有效、选择性、可口服、可透过血脑屏障的T型电压门控钙通道(T-typecalciumchannel)阻滞剂，对Cav3.1，Cav3.2，Cav3.3，Cav1.2的IC50值分别为6.4，18，7.5和2410nM。ACT-709478对大鼠、小鼠、狗和猕猴的T-typecalciumchannel都有作用，物种差异不大。ACT-709478可用于全身性癫痫的研究。
CAS：1838651-58-3
分子式：C22H18F3N5O
分子量：425.41
纯度：98%
存储：Store at -20°C

Background:

ACT-709478 is a potent, selective, oral active, and brain penetrating T-type calcium channel blocker, with IC50s of 6.4, 18, 7.5 and 2410 nM for Cav3.1, Cav3.2, Cav3.3, Cav1.2, respectively. ACT-709478 is effective on rat and mice, dog, and cynomolgus T-type calcium channel, with no significant species differences. ACT-709478 is used in the research of generalized epilepsies[1].

ACT-709478 (Compound 66b) blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1].ACT-709478 shows weak inhibition on P450, with IC50s of 52, 14, 22, 25, 15, and 51 μM for P4502A6, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4, respectively[1].

[1]. Bezen?on O, et al. Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem. 2017 Dec 14;60(23):9769-9789.