GNE-0439 is a novel Nav1.7-selective inhibitor with IC 50 of 0.34 uM and inhibits Nav1.5 with an IC 50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC 50 =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.
性状
Solid
IC50 & Target[1][2]
IC50: 0.34 uM (Nav1.7)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 200 mg/mL (578.90 mM; Need ultrasonic)配制储备液
[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.