ACT-709478 (Synonyms: ACT-709478) |
| Catalog No.GC31100 |
ACT-709478은 강력하고 선택적이며 경구 활성이며 뇌를 관통하는 T형 칼슘 채널 차단제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1838651-58-3
Sample solution is provided at 25 µL, 10mM.
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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.
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