Overview
- Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405.
- Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540.
- Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875.
Centrifuge all product preparations before use (10000 x g 5 min).
Alomone Labs PF-05089771 blocks NaV1.7 channels expressed in Xenopus oocytes.A. Time course of PF-05089771 (#P-315) inhibition of NaV1.7 channels current. Membrane potential was held at -100 mV, current was elicited by a 100 ms voltage step to 0 mV every 2 sec, and gradually inhibited by 200 nM PF-05089771 (bar) over the course of 10 min of application. B. Superimposed traces of NaV1.7 channels current upon application of control and of 200 nM PF-05089771 (as indicated).
- Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405.
- Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540.
- Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875.
- Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
PF-05089771 is a synthetic arylsulfonamide compound that acts as a potent, state dependent and selective inhibitor of human NaV1.7 channel.
PF-05089771 interacts with the voltage-sensor domain (VSD) of domain IV of the channel and demonstrates a strong preference for inactivated channels with inhibition that develops in a slow rate1,2. It inhibits half-inactivated human NaV1.7 channels with an IC50 of 11 nM and an IC50 of ~10 μM for resting channels1. The compound is currently being used to explore the NaV1.7 channel blockade for the treatment of acute or chronic pain conditions3,4.
NaV1.7 channel plays an important role in the human pain signaling pathway and it is an important therapeutic target for treatment of chronic pain.
PF-05089771 (#P-315) is a highly pure, synthetic, and biologically active compound.
Powered by Bioz
