ACT 709478

Modify Date: 2024-01-19 13:27:57

ACT 709478 Structure
ACT 709478 structure
Common Name ACT 709478
CAS Number 1838651-58-3 Molecular Weight 425.41
Density N/A Boiling Point N/A
Molecular Formula C22H18F3N5O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ACT 709478


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].

 Names

Name ACT-709478

 ACT 709478 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C22H18F3N5O
Molecular Weight 425.41
Storage condition 2-8℃