NaV1.7-Compound 36

4-(5-Chloro-6-(2,5-difluorophenoxy)-3-pyridinyl)-2-fluoro-5-methoxy-N-(methylsulfonyl)benzamide
A Potent and Selective Blocker of NaV1.7 Channels
    Cat #: CMN-003
    Alternative Name 4-(5-Chloro-6-(2,5-difluorophenoxy)-3-pyridinyl)-2-fluoro-5-methoxy-N-(methylsulfonyl)benzamide
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic.
    MW: 486.85
    Purity: >99% (HPLC)
    Effective concentration 50 nM – 50 µM.
    Structure
    • NaV1.7-Compound 36
    Chemical name 4-(5-Chloro-6-(2,5-difluorophenoxy)-3-pyridinyl)-2-fluoro-5-methoxy-N-(methylsulfonyl)benzamide.
    Molecular formula C20H14ClF3N2O5S.
    Activity NaV1.7-Compound 36 is a potent and selective blocker of NaV1.7 channels. It inhibits human NaV1.7 with IC50 of 69 nM. Compound 36 is selective for NaV1.7 over other human NaV isoforms and important targets, such as hERG1.
    References-Activity
    1. DiMauro, E.F. et al. (2016) J. Med. Chem. 59, 7818.
    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 up to 200 mM in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • NaV1.7-Compound 36
      Alomone Labs NaV1.7-Compound 36 blocks NaV1.7 channels expressed in Xenopus oocytes.
      A. Representative time course of NaV1.7-Compound 36 (#CMN-003) inhibition of NaV1.7 channel peak 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 10 µM and 50 µM NaV1.7-Compound 36 application (horizontal bars). B. Superimposed traces of NaV1.7 current upon application of control and of 10 µM and 50 µM NaV1.7-Compound 36, as indicated.
    References - Scientific background
    1. DiMauro, E.F. et al. (2016) J. Med. Chem. 59, 7818.
    2. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    NaV1.7-Compound 36 is a potent and selective blocker of NaV1.7 channels. NaV1.7-Compound 36 inhibits human NaV1.7 channels with IC50 value of 69 nM1.

    There are nine mammalian subtypes of NaV channels: NaV1.1–NaV1.9. They are essential for the initiation of action potentials in excitable cells and are considered to be important therapeutic targets for numerous pathophysiological conditions such as cardiac arrhythmia, and epilepsy. NaV1.7 channel plays an important role in nociception and it is an important therapeutic target in chronic pain1,2.

    Target NaV1.7 channels
    Last update: 24/01/2020

    NaV1.7-Compound 36 (#CMN-003) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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