PF-05186462

A Potent and Selective Blocker of NaV1.7 Channels
  • New
Cat #: P-365
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source Synthetic
    MW: 531.89
    Purity: >96%
    Effective concentration 20 nM – 5 µM.
    Structure
    Chemical name 5-chloro-2-fluoro-4-(2-(pyridazin-4-yl)-4-(trifluoromethyl)phenoxy)-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide.
    Molecular formula C19H10ClF4N5O3S2.
    CAS No.: 1235406-03-7
    Activity PF-05186462 is a potent and selective blocker of NaV1.7 channels, shown to inhibit human NaV1.7 channels with IC50 of 21 nM, and tested for clinical application in human microdose studies1.
    Storage before reconstitution Store at -20°C.
    Reconstitution Soluble up to 200 mM in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage after reconstitution Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    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.
    References
    1. Jones, H.M. et al. (2016) Clin. Pharmacokinet. 55, 875.
    2. Klint, J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    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.

    Target NaV1.7 channels

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    Last update: 20/09/2018

    PF-05186462 (#P-365) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use