1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Nav1.1 activator 1

Nav1.1 activator 1 

Cat. No.: HY-126429
Handling Instructions

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.

For research use only. We do not sell to patients.

Nav1.1 activator 1 Chemical Structure

Nav1.1 activator 1 Chemical Structure

CAS No. : 2332897-85-3

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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].

IC50 & 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.
Molecular Weight

440.46

Formula

C₂₄H₂₃F₃N₄O

CAS No.

2332897-85-3

SMILES

O=C(C1=C(C2=CC(F)=CC=C2F)C=CN=C1N3C[[email protected]@H](F)CC3)NC4=CC=C(C(C)C)N=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Nav1.1 activator 1Sodium ChannelNa channelsNa+ channelsBBBDravetsyndromecurrent,Inhibitorinhibitorinhibit

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Nav1.1 activator 1
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HY-126429
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