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NS-1619

Selective and Potent Enhancer of KCa1.1 Channels and an Inhibitor of SERCA Pumps

Cat #: N-105
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 362.2
    Purity: >95%
    Effective concentration 100 nM - 100 μM.
    Structure
    Chemical name 1,3-Dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one.
    Molecular formula C15H8F6N2O2.
    CAS No.: 153587-01-0
    Activity NS-1619 is a potent and selective KCa1.1 (BK, slo, Large conductance Ca2+-activated K+) channel modulator (enhancer)1. NS-1619 was effective in eliciting and enhancing KCa1.1 channels in smooth muscle as well as in neurons with maximal effects at concentrations around 30 μM1,2. NS-1619 was used in vivo by intracarotid infusion and significantly enhanced blood tumor barrier permeability in the brain tumor area but not in normal brain tissue3.
    References-Activity
    1. Edwards, G. et al. (1994) Br. J. Pharmacol. 113, 1538.
    2. Sellers, A.G. and Ashford, L.M.J. (1994) Br. J. Pharmacol. 113, 659.
    3. Ningaraj, N.S. et al. (2002) J. Pharmacol. Exp. Ther. 301, 838.
    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-1619 enhances KCa1.1 currents in Xenopus oocytes.
      Alomone Labs NS-1619 enhances KCa1.1 currents in Xenopus oocytes.
      A. Families of KCa1.1 channel current responses to increasing voltage step stimulation (from -50 mV to + 50 mV), before (left) and during (right) application of 100 μM NS-1619 (#N-105). Currents were elicited by 100 ms voltage step from -100 mV applied every 10 sec. B. Time course of current amplitude at 0 mV before, during application of 100 μM NS-1619 (green) and upon wash, demonstrating the current amplitude enhancement. C. Voltage dependence of KCa1.1 channel activity enhancement.
    References - Scientific background
    1. Andersson K.E. et al. (2004) Physiol. Rev. 84, 935.
    2. Heppner, T.J. et al. (1997) Am. J. Physiol. 273, C110.
    3. Salkoff, L. et al. (2006) Nat. Rev. Neurosci. 7, 921.
    4. Olesen S.P. et al. (1994) Eur. J. Pharmacol. 251, 53.
    5. Holland M. et al. (1996) Br. J. Pharmacol. 117, 119.
    6. Macmillan S. et al. (1995) Br. J. Pharmacol. 116, 1656.
    7. Yamamura H. et al. (2001) Br. J. Pharmacol. 132, 828.
    8. Han X. et al. (2008) Biochem. Biophys. Res. Commun. 375, 205.
    9. Wrzosek, A. (2014) Cell Calcium 56, 14.
    Scientific background

    The large conductance voltage- and Ca2+-activated K+ (BK) channels, also known as BKCa, KCa1.1, Slo, or MaxiK, play an important role in modulating nerve and muscle cell contractility and excitability1-3. BK channels are activated by both depolarizing voltages and by an increase in intracellular free Ca2+, thus coupling the membrane potential to intracellular signaling.

    NS-1619 is a potent and selective KCa1.1 channel modulator (enhancer)4. It has the potential to modulate cell excitability in neurons and smooth muscle5-7. The effect of relaxation of NS-1619 on the BK channel in smooth muscle cells has an EC50 of 10–30 µM. It is also dose-dependent, resulting in a shift of the activation curve by up to -50 mV towards negative membrane potentials, but fully reversible8.

    NS-1619 also modulates intracellular Ca2+ by inhibiting SERCA pumps9.

    Target KCa1.1 K+ channels, SERCA pumps
    Lyophilized Powder
    Last update: 06/11/2022

    NS-1619 (#N-105) 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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