- Jones, H.M. et al. (2016) Clin. Pharmacokinet. 55, 875.
- Alomone Labs PF-05186462 blocks NaV1.7 channels expressed in Xenopus oocytes.A. Representative time course of PF-05186462 (#P-365) inhibition of NaV1.7 channel currents. Membrane potential was held at -100 mV. Current was elicited by a 100 ms voltage step to 0 mV every 10 sec and inhibited by 1 µM and 5 µM PF-05186462 application (horizontal bars). B. Superimposed traces of NaV1.7 current upon application of control and of 1 µM and 5 µM PF-05186462, as indicated.
PF-05186462 is a potent and selective NaV1.7 channel blocker displaying IC50 values of 21 nM for human NaV1.71.
There are nine mammalian NaV channel subtypes: NaV1.1–NaV1.9. These channels are essential for action potential initiation and upstroke in excitable cells and are considered to be important therapeutic targets for numerous pathophysiological conditions such as cardiac arrhythmia, and epilepsy1,2.
NaV1.7 channel plays an important role in the human pain signaling pathway and it is an important therapeutic target for treatment of chronic pain1,2.
PF-05186462 (#P-365) is a highly pure, synthetic, and biologically active compound.