Nav1.1 activator 1

Modify Date: 2024-01-12 11:08:37

Nav1.1 activator 1 Structure
Nav1.1 activator 1 structure
Common Name Nav1.1 activator 1
CAS Number 2332897-85-3 Molecular Weight 440.46
Density N/A Boiling Point N/A
Molecular Formula C24H23F3N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Nav1.1 activator 1


Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6[1].

 Names

Name Nav1.1 activator 1

 Nav1.1 activator 1 Biological Activity

Description Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6[1].
Related Catalog
Target

Nav1.1[1].

In Vivo Nav1.1 activator 1 (compound 4) is a valuable Nav1.1 activator for further evaluation of pathophysiological functions of the Nav1.1 channel and has potential for therapeutic treatments of CNS diseases such as Dravet syndrome[1]. Animal Model: Mice[1]. Dosage: 30 mg/kg (Pharmacokinetic Analysis). Administration: IP once (Exposure was measured at 1 h after administration). Result: Intraperitoneal administration (30 mg/kg) of compound resulted in sufficient brain exposure (193 ng/g 1 h after administration), which corresponded to 13 nM of free brain concentration comparable to the in vitro potency of the compound. Had a potential use as an in vivo tool to investigate whether this type of Nav1.1 activator can restore Nav1.1 functions and modify the disease state in animal models. Could penetrate the blood-brain barrier (BBB) in humans.
References

[1]. Miyazaki T, et al. Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Bioorg Med Chem Lett. 2019 Mar 15;29(6):815-820.

 Chemical & Physical Properties

Molecular Formula C24H23F3N4O
Molecular Weight 440.46