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

Nav1.1 activator 1 

Cat. No.: HY-126429 Purity: 98.25%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (567.59 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2704 mL 11.3518 mL 22.7035 mL
5 mM 0.4541 mL 2.2704 mL 4.5407 mL
10 mM 0.2270 mL 1.1352 mL 2.2704 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.72 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.25%

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

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

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Nav1.1 activator 1
Cat. No.:
HY-126429
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