Nav1.1 activator 1

Name: Nav1.1 activator 1
Brand: MedChemExpress
SKU: HY-126429
Rating: 4.5 (1 reviews)

Cat. No.: HY-126429 Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Nav1.1 activator 1 (compound 4), a highly potent Na_v1.1 activator with BBB penetration, increases decay time constant (tau) of Na_v1.1 currents at 0.03 μM along with significant selectivity against Na_v1.2, Na_v1.5, and Na_v1.6.

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

Nav1.1 activator 1 Chemical Structure

CAS No. : 2332897-85-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 341	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 341	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Na_v1.1^[1].

In Vivo

Nav1.1 activator 1 (compound 4) is a valuable Na_v1.1 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].

MedChemExpress (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 Na_v1.1 activator can restore Na_v1.1 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

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (567.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) HNMR (215 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2704 mL	11.3518 mL	22.7035 mL	56.7588 mL
	5 mM	0.4541 mL	2.2704 mL	4.5407 mL	11.3518 mL
	10 mM	0.2270 mL	1.1352 mL	2.2704 mL	5.6759 mL
	15 mM	0.1514 mL	0.7568 mL	1.5136 mL	3.7839 mL
	20 mM	0.1135 mL	0.5676 mL	1.1352 mL	2.8379 mL
	25 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2704 mL
	30 mM	0.0757 mL	0.3784 mL	0.7568 mL	1.8920 mL
	40 mM	0.0568 mL	0.2838 mL	0.5676 mL	1.4190 mL
	50 mM	0.0454 mL	0.2270 mL	0.4541 mL	1.1352 mL
	60 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9460 mL
	80 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7095 mL
	100 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5676 mL