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GNE-131

Chemical Structure : GNE-131

CAS No.: 1629063-81-5

GNE-131 (GNE131)

Catalog No.: PC-35103Not For Human Use, Lab Use Only.

GNE-131 is a potent, selective inhibitor of sodium channel NaV1.7 with IC50 of 3 nM, >80-fold selectivity over the cardiac sodium channel NaV1.5.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-131 is a potent, selective inhibitor of sodium channel NaV1.7 with IC50 of 3 nM, >80-fold selectivity over the cardiac sodium channel NaV1.5.
GNE-131 demonstrates effects on mouse NaV1.7 using the Qube automated electrophysiology platform with IC50 of 7 nM.
GNE-131 shows significant reduction of nociceptive behavior on aconitine-induced pain in transgenic IEM mice, with up to 85% reduction at the 30 mg/kg dose and a plasma concentration of 2.8 uM.

Physicochemical Properties

M.Wt 442.578
Formula C23H30N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(7-(Adamantan-1-ylmethoxy)-6-cyclopropyl-[1,2,4]triazolo[4,3-a]-pyridin-3-yl)cyclopropanesulfonamide

References

1. Focken T, et al. J Med Chem. 2018 May 23. doi: 10.1021/acs.jmedchem.7b01826.

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