| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.34 uM (Nav1.7) | ||||||||||||
| Name | GNE-0439 | ||||||||||||
| CAS | 1241902-40-8 | ||||||||||||
| Formula | C21H31NO3 | ||||||||||||
| Molar Mass | 345.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |