GNE-0439

GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders[1].

Product Specifications

CAS Number

[1241902-40-8]

UNSPSC

12352005

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gne-0439.html

Purity

99.11

Solubility

DMSO : 130 mg/mL (ultrasonic)

Smiles

CC(C)[C@@H](C(O)=O)NC(C1=CC=C(C2CCC(CCC)CC2)C=C1)=O

Molecular Formula

C21H31NO3

Molecular Weight

345.48

References & Citations

[1]Chernov-Rogan T, et al. Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors. Proc Natl Acad Sci U S A. 2018 Jan 23;115 (4) :E792-E801.