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NS8593

A Blocker of KCa2 and TRPM7 Channels

Cat #: N-196
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 263.3
    Purity: >98.5%
    Effective concentration 100 nM -10 µM.
    Structure
    Chemical name N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-1H-benzimidazol-2-amine.
    Molecular formula C17H17N3.
    CAS No.: 875755-39-8
    PubChem CID 11587013
    Activity NS8593 is KCa2 (SK) channel blocker, with no activity towards KCa3.1 channels, with IC50~100 nM1,2. It also blocks TRPM7 channels3.
    References-Activity
    1. Jenkins, D.P. et al. (2011) Mol. Pharmacol. 79, 899.
    2. Strobaek, D. et al. (2006) Mol. Pharmacol. 70, 1771.
    3. Chubanov, V. et al. (2012) Br. J. Pharmacol. 166, 1357.
    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 100mM 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 NS8593 blocks KCa2.2 (SK2) currents expressed in HEK 293T cells.
      Alomone Labs NS8593 blocks KCa2.2 (SK2) currents expressed in HEK 293T cells.
      A. Time course of KCa2.2 current amplitude and its inhibition by 2 and 10 µM NS8593 (#N-196). Currents were elicited by application of voltage ramp from a holding potential of -100 mV to +60 mV (150 msec), delivered every 10 seconds. B. Superimposed example traces of current responses before and during perfusion of 2 and 10 µM NS8593 as indicated.
    References - Scientific background
    1. Strobaek, D. et al. (2006) Mol. Pharmacol. 70, 1771.
    2. Jenkins, D.P. et al. (2011) Mol. Pharmacol. 79, 899.
    3. Chubanov, V. et al. (2012) Br. J. Pharmacol. 166, 1357.
    Scientific background

    NS8593 inhibits the gating modulation of all SK, small conductance Ca2+-activated K+ channels (KCa2.1, KCa2.2, KCa2.3) and blocks SK3 channels with an IC50 of 104 nM1,2. It does so by shifting the apparent Ca2+-dependence to higher Ca2+ concentrations2. NS8593 has no effect on other KCa channels1.

    NS8593 was also found to block TRPM7 currents with an IC50 value of 1.6 μM.

    Target SK K+ channels, TRPM7
    Lyophilized Powder
    Last update: 11/04/2021

    NS8593 (#N-196) 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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