GNE-616

Name: GNE-616
Brand: TargetMol
SKU: T11439
Rating: 4.5 (1 reviews)

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Catalog No. T11439Cas No. 2349371-81-7

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.

GNE-616

😃Good

Catalog No. T11439Cas No. 2349371-81-7

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,720	3-6 months	3-6 months
50 mg	$3,580	3-6 months	3-6 months
100 mg	$4,900	3-6 months	3-6 months

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

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Product Introduction

Bioactivity

Description	GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.
Targets&IC50	Nav1.2 (human):12 nM (ki), Nav1.6 (human):29 nM (ki), Nav1.7 (human): kd:0.38 nM , Nav1.7 (human):ki:0.79 nM
In vitro	Site-directed mutagenesis is essential for determining the isoform selectivity profile of GNE-616.
In vivo	GNE-616 demonstrates significant activity in a Nav1.7-dependent inherited erythromelalgia (IEM) PK/PD model.

Chemical Properties

Molecular Weight	537.53
Formula	C₂₄H₂₃F₄N₅O₃S
Cas No.	2349371-81-7
Smiles	C(F)(F)(F)[C@@H]1C[C@@H](N(CC1)[C@@H]2C=3C(=CC(S(NC=4C=CN=CN4)(=O)=O)=C(F)C3)OCC2)C5=CC=CC=N5
Relative Density.	no data available

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.

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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.

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