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NS-3623

An Opener of KV11.1 (hERG) Channels

Cat #: N-190
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 427.18
    Purity: >95%
    Form Lyophilized powder.
    Effective concentration 10-200 µM.
    Structure
    Chemical name N-(4-bromo-2-(1H-tetrazol-5-yl)phenyl)-N’-(3-trifluoromethyl-phenyl)urea.
    Molecular formula C15H10BrF3N6O.
    CAS No.: 343630-41-1
    Activity NS-3623 is an opener of KV11.1 channels with an EC50 of 10.5 μM1.
    References-Activity
    1. Hansen, R.S. et al. (2006) Mol. Pharmacol. 70, 1319.
    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 DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs NS-3623 reversibly enhances KV11.1 (hERG) channels heterologously expressed in HEK-293 cells.
      Alomone Labs NS-3623 reversibly enhances KV11.1 (hERG) channels heterologously expressed in HEK-293 cells.
      A. Time course of the reversible enhancing effect of 100 µM NS-3623 (#N-190) on hERG currents, elicited by a 250 ms voltage step from the holding potential of -100 mV to 40 mV, followed by a 250 ms step to -20 mV, applied every 10 s. Current amplitude was measured at the end of the pulse to -20 mV (see large outward tail in B). B. Superimposed traces of channel activity before and during applications of the indicated NS-3623 concentrations (taken from the experiment shown in panel A).
    References - Scientific background
    1. Sanguinetti, M.C. et al. (1995) Cell 81, 299.
    2. Akar, F.G. (2010) J. Cardiovasc. Electrophysiol. 21, 930.
    3. Hansen, R.S. et al. (2006) Mol. Pharmacol. 70, 1319.
    4. Hansen, R.S. et al. (2006) Mol. Pharmacol 69, 266.
    Scientific background The hERG (KV11.1) potassium channel underlies the rapid delayed rectifier current, IKr, which is a major determinant of cardiac repolarization1. IKr strongly modulates action potential duration (APD) and the QT interval at the cellular and organ levels, respectively. Loss of function mutations in hERG results in altered channel gating or impaired intracellular trafficking and reduced cell surface expression. These molecular defects give rise to a congenital form of the long-QT Syndrome type 2 (LQT2) and its associated arrhythmia, torsade de pointes (TdP)2. Recent studies have focused on the use of hERG channel agonists, such as NS-3623, as potential drug candidates for the treatment of cardiac arrhythmic disorders 3. The molecular mechanism of action NS-3623 is to primarily activate the native HERG channels underlying the IKr of the cardiomyocytes with an EC50 value of 10.5 μM4.
    Target hERG K+ channels
    Lyophilized Powder
    Last update: 06/11/2022

    NS-3623 (#N-190) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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