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PF-05241328

A Potent and Selective Blocker of NaV1.7 Channels

Cat #: P-345
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 436.91
    Purity: >99%
    Effective concentration 50 nM – 50 µM.
    Structure
    Chemical name 1-[5-chloro-6-(2-methylpropoxy)pyridin-3-yl]-3-methyl-N-methylsulfonylindazole-5-carboxamide.
    Molecular formula C19H21ClN4O4S.
    CAS No.: 1387633-03-5
    PubChem CID 68109743
    Activity PF-05241328 is a potent and selective blocker of NaV1.7 channels, shown to inhibit human NaV1.7 channels with IC50 of 31 nM, and tested for clinical application in human microdose studies1.
    References-Activity
    1. 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 Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs PF-05241328 blocks NaV1.7 channels expressed in Xenopus oocytes.
      Alomone Labs PF-05241328 blocks NaV1.7 channels expressed in Xenopus oocytes.
      A. Representative time course of PF-05241328 (#P-345) inhibition of NaV1.7 channel current. 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 10 µM and 50 µM PF-05241328 application (horizontal bars). B. Superimposed traces of NaV1.7 current upon application of control and of 10 µM and 50 µM PF-05241358, as indicated.
    References - Scientific background
    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-05241328 a potent and selective blocker of NaV1.7 channels with IC50 value of 31 nM1. PF-05089771 is being used to explore the NaV1.7 channel blockade for the treatment of acute or chronic pain conditions1,2.

    NaV1.7 channel plays an important role in the human pain signaling pathway and it is an important therapeutic target for treatment of chronic pain.

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

    PF-05241328 (#P-345) 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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