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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	Availability
25 mg	$3,170	10-14 weeks
50 mg	$4,180	10-14 weeks
100 mg	$5,800	10-14 weeks

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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	Nav1.6 (human):29 nM (ki), Nav1.2 (human):12 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
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.

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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Keywords

hNav1.7hNav1.6hNav1.2GNE-616GNE616GNE 616