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NS-6180

A Potent Blocker of KCa3.1 Channel

Cat #: N-230
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 323.3
    Purity: >98%
    Effective concentration 10 nM – 1 μM.
    Structure
    Chemical name 4-[[3-(Trifluoromethyl)phenyl]methy­l]-2H-1,4-benzothiazin-3(4H)-one.
    Molecular formula C16H12F3NOS.
    CAS No.: 353262-04-1
    Activity NS-6180 blocks SK4 channels with IC50 of  9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels respectively1.
    References-Activity
    1. Strøbæk, D. et al. (2013) Br. J. Pharmacol. 168, 432.
    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 NS-6180  blocks KCa3.1 currents expressed in HEK 293T cells.
      Alomone Labs NS-6180  blocks KCa3.1 currents expressed in HEK 293T cells.
      A. Time course of KCa3.1 current amplitude without and with 100 nM NS-6180 (#N-230). Currents were elicited by application of voltage ramp from -120 mV to +60 mV (150 msec), delivered every 10 seconds, holding potential of -80 mV. B. Superimposed example traces of current responses before and during perfusion of 100 nM NS-6180 as indicated.
    References - Scientific background
    1. Strøbæk, D. et al. (2013) Br. J. Pharmacol. 168, 432.
    2. Koshy, S. et al. (2013) PLoS One. 8, e76740.
    Scientific background

    The benzothiazinone NS-6180 is a potent and selective KCa3.1 channel blocker1.

    The Ca2+-activated K+ channel, KCa3.1, plays a major role in the controlled expression of essential genes orchestrating proliferation, migration and cytokine production by participating in the regulation of calcium entry. A highly regulated and sustained increase in cytosolic Ca2+ is critical in these processes thus, the KCa3.1 channel is a potential target for therapy of immune disease1.

    Inhibition of KCa3.1 channel by NS-6180 demonstrates IC50 value of 14 nM in human, 9 nM in rat and 15 nM in mouse. NS6180 also has the ability to inhibit KCa1.1, KV1.3 and KV11.1 channels with IC50s above 10 µM2.

    Target KCa3.1 channels
    Lyophilized Powder
    Last update: 08/06/2021

    NS-6180 (#N-230) 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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