1838651-58-3

1838651-58-3 structure

Name: ACT 709478
Chemical Name: ACT-709478
CAS Number: 1838651-58-3
Molecular Formula: C₂₂H₁₈F₃N₅O
Molecular Weight: 425.41
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2019-03-31 00:21:34
Modify Date: 2024-01-19 13:27:57
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].

Name	ACT-709478

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Neurological Disease
Target	Cav3.1:6.4 nM (IC50) Cav3.2:18 nM (IC50) Cav3.3:7.5 nM (IC50) Cav1.2:2410 nM (IC50)
In Vitro	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].
References	[1]. Bezençon 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.