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GNE-616

GNE-616
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.
Catalog No. T11439Cas No. 2349371-81-7
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GNE-616

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.
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.
Pack SizePriceAvailabilityQuantity
25 mg$3,17010-14 weeks
50 mg$4,18010-14 weeks
100 mg$5,80010-14 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
Nav1.2 (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 Weight537.53
FormulaC24H23F4N5O3S
Cas No.2349371-81-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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