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NS-11021

1AOB1480, SYN5051

A Potent and Selective Activator of KCa1.1 Channel and KCNQ4 Channel at High Concentrations

Cat #: N-335
Alternative Name 1AOB1480, SYN5051
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 511.24
    Purity: >99%
    Effective concentration 0.5-50 µM.
    Structure
    Chemical name 1-[3,5-bis(trifluoromethyl)phenyl]-3-[4-bromo-2-(2H-tetrazol-5-yl)phenyl]thiourea.
    Molecular formula C16H9BrF6N6S.
    CAS No.: 956014-19-0
    PubChem CID 24825677
    Activity NS-11021 is a potent KCa1.1 channel agonist, enhancing KCa1.1 currents with EC50 of 0.4 µM, whilst having no effect on a variety of K+, Na+ and Ca2+ channels at 10 µM1.
    References-Activity
    1. Bentzen, B.H. et al. (2007) Mol. Pharmacol. 72, 1033.
    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 Up to 100 mM in 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-11021 activates KCa1.1 channels expressed in Xenopus oocytes.
      Alomone Labs NS-11021 activates KCa1.1 channels expressed in Xenopus oocytes.
      A. Time course of normalized KCa1.1 currents at +50 mV. Currents were elicited by 150 ms voltage ramp from holding potential of -100 mV to +100 mV every 10 sec. NS-11021 (#N-335), applied at 2 µM and 10 µM, as indicated (bars), reversibly enhanced KCa1.1 currents. B. Current traces upon application of control, or of  2 µM and 10 µM NS-11021 (as indicated).
    References - Scientific background
    1. Bentzen, B.H. et al. (2007) Mol. Pharmacol. 72, 1033.
    Scientific background

    NS-11021 is a synthetic, potent and selective activator of KCa1.1 - the large conductance Ca2+-activated K+-channel with an EC50 value of 0.4 µM KCa1.1. NS-11021 affects KCa1.1 in both their open and closed states. Application of NS-11021 (3 µM) increased Kca1.1 currents by 171±31% for channels that shift between open and closed state and by 187±27% for channels kept in closed conformation in Xenopus oocytes heterologously expressing hKCa1.1. NS-11021 also produces a negative shift in the threshold for current activation and increases the peak tail current amplitude for KCa1.1 channels. NS-11021 also activates the KCNQ4 (KV7.4) channel at high concentrations but has a minor or no effect on other potassium and calcium channels. NS-11021 is effective when exposed to either side of the cell’s membrane and most likely exerts its effect through direct binding to the KCa1.1 α-subunit1.

    Target KCa1.1, KCNQ4 channels
    Lyophilized Powder
    Last update: 02/01/2022

    NS-11021 (#N-335) 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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