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

Nav1.1 activator 1 

目录号: HY-126429 纯度: 98.25%
产品使用指南

Nav1.1 activator 1 (compound 4) 是强有效的、能透过血脑屏障的、 Nav1.1 激动剂,0.03 μM 可增加衰减Nav1.1 电流的时间常数 τ。对 Nav1.2、Nav1.5、Nav1.6 有显著的选择性。

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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[C@@H](F)CC3)NC4=CC=C(C(C)C)N=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

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产品名称:
Nav1.1 activator 1
目录号:
HY-126429
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