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PF-05089771

A Potent and Selective Blocker of NaV1.7 Channel

Cat #: P-315
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 500.34
    Purity: >97%
    Effective concentration 10 nM – 1 µM.
    Structure
    Chemical name 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide.
    Molecular formula C18H12Cl2FN5O3S2.
    CAS No.: 1235403-62-9
    PubChem CID 46840946
    Activity PF-05089771 is a novel, potent, state-dependent and selective inhibitor of NaV1.7, shown to inhibit half-inactivated human NaV1.7 channels with IC50 of 11 nM via interaction with the domain IV, and tested for clinical application in human microdose studies1-3.
    References-Activity
    1. Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405.
    2. Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540.
    3. Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 50 mM in DMSO, also soluble in methanol.
    Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs PF-05089771 blocks NaV1.7 channels expressed in Xenopus oocytes.
      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).
    References - Scientific background
    1. Alexandrou, A.J. et al. (2016) PLoS ONE 11, e0152405.
    2. Theile, J.W. et al. (2016) Mol. Pharmacol. 90, 540.
    3. Jones, H.M. et al. (2016) Clin Pharmacokinet. 55, 875.
    4. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    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.

    Target NaV1.7 channels
    Lyophilized Powder
    Last update: 06/11/2022

    PF-05089771 (#P-315) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
    Shipping and Ordering information

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