Nav1.1 activator 1 - 10mM in DMSO , CAS No.2332897-85-3

CAS: 2332897-85-3 Cat. No.: N655081 Molecular Weight: 440.46

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Nav1.1 activator 1 (compound 4), a highly potent Na v 1.1 activator with BBB penetration , increases decay time constant (tau) of Na v 1.1 currents at 0.03 μM along with significant selectivity against Na v 1.2, Na v 1.5, and Na v 1.6

In Vivo

Nav1.1 activator 1 (compound 4) is a valuable Na v 1.1 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice . 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 Na v 1.1 activator can restore Na v 1.1 functions and modify the disease state in animal models. Could penetrate the blood-brain barrier (BBB) in humans.

IC50& Target:Na v 1.1

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Nav1.1 activator 1 (compound 4), a highly potent Na v 1.1 activator with BBB penetration , increases decay time constant (tau) of Na v 1.1 currents at 0.03 μM along with significant selectivity against Na v 1.2, Na v 1.5, and Na v 1.6.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ACTIVATOR

Names and Identifiers

• Molecular Weight: 440.46