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NaV1.7 inhibitor-1

Name: NaV1.7 inhibitor-1
Brand: TargetMol
SKU: T12181
Price: 106 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12181Cas No. 1494585-79-3

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

NaV1.7 inhibitor-1

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Purity: 99.89%

Catalog No. T12181Cas No. 1494585-79-3

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$106	In Stock	In Stock
5 mg	$268	In Stock	In Stock
10 mg	$428	In Stock	In Stock
25 mg	$737	In Stock	In Stock
50 mg	$987	In Stock	In Stock
100 mg	$1,450	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$295	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.89%

Appearance:solid

Color:White

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COA HNMR LCMS

Product Introduction

NaV1.7 inhibitor-1 AI Summary

NaV1.7 inhibitor-1 is a potent inhibitor of voltage-gated sodium channels (NaV's), especially highlighting significant activity against Nav1.7. The compound demonstrates very low IC50 values ranging from 0.6 to 50.0 nM across several sodium channel subtypes (Nav1.1, Nav1.2, Nav1.5, Nav1.6, and Nav1.7), with selectivity indices emphasizing a strong preference for Nav1.7 compared to others. Specifically, the IC50 for Nav1.7 inhibition is 2.2 nM in mice and 3.7 nM in rats. Furthermore, electrophysiological assays revealed an IC50 of 4.0 nM, while radioligand binding studies indicated an IC50 of 3.0 nM, corroborating its high affinity for sodium channels. In vivo studies illustrate its antinociceptive effects in mouse models of pain and erythromelalgia, reducing nociceptive behavior in a dose-dependent manner. The compound also boasts good oral bioavailability and favorable pharmacokinetics, including a reasonable half-life, clearance, and volume of distribution, with a low unbound fraction in mouse plasma..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).
Targets&IC50	Nav1.7 (human):0.6 nM

Chemical Properties

Molecular Weight	435.55
Formula	C₂₃H₃₀FNO₄S
Cas No.	1494585-79-3
Smiles	CC1(COc2cc(F)c(cc2C2CC2)C(=O)NS(=O)(=O)C2CC2)CCC2(CC2)CC1
Relative Density.	1.32 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (206.64 mM), Sonication and heating to 60℃ are recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2959 mL	11.4797 mL	22.9595 mL	114.7974 mL
5 mM	0.4592 mL	2.2959 mL	4.5919 mL	22.9595 mL
10 mM	0.2296 mL	1.1480 mL	2.2959 mL	11.4797 mL
20 mM	0.1148 mL	0.5740 mL	1.1480 mL	5.7399 mL
50 mM	0.0459 mL	0.2296 mL	0.4592 mL	2.2959 mL
100 mM	0.0230 mL	0.1148 mL	0.2296 mL	1.1480 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc