A Selective and Potent Activator of KCa2.2 and KCa2.3 Channels and a Blocker of TRPM7 Channels
    Cat #: C-110
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 285.4
    Purity: >98%
    Effective concentration 1-100 μM.
    • CyPPA
    Chemical name N-Cyclohexyl-N-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-4-pyrimidinamine.
    Molecular formula C16H23N5.
    CAS No.: 73029-73-9.
    Activity CyPPA is an activator of small conductance Ca2+-activated K+ channels KCa2.2 (SK2) and KCa2.3 (SK3) with EC50 values of 5.6 and 14 μM for SK3 and SK2 respectively. It displays no activity at SK1 and intermediate conductance KCa (IK) channels1. CyPPA blocks TRPM7 channels2.
    1. Hougaard, C. et al. (2007) Br J. Pharmacol. 151, 655.
    2. 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 DMSO or ethanol. 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
    • CyPPA
      Alomone Labs CyPPA enhances hSK2 channel currents in transiently transfected HEK293T cells.
      Cells were stimulated with 100 μM CyPPA (#C-110) and currents were measured using whole cell voltage-clamp. A. Time course at -20mV showing the effect of 100 μM CyPPA and its inhibition with 150 nM Apamin (#STA-200). B. Representative currents at control conditions (bottom) and following application of 100 μM CyPPA (top). Currents were elicited by a 150 ms voltage ramp from -120 to 60 mV every 10 seconds from a holding potential of -80 mV (current responses are shown between -120 and -10 mV). Leaks were subtracted offline.
    References - Scientific background
    1. Kohler, M. et al. (1996) Science 273, 1709.
    2. Stocker, M. et al. (2000) Mol Cell Neurosci. 15, 476.
    3. Hougaard, C. et al. (2007) Br J. Pharmacol. 151, 655.
    4. Seutin, V. et al. (2007) Br J. Pharmacol. 151, 568.
    5. Chubanov, V. et al. (2012) Br. J. Pharmacol. 166, 1357.
    Scientific background

    Ca2+-activated potassium channels (KCa) are a group of 6/7-TM ion channels that selectively transport K+ ions across biological membranes. They are broadly classified into three subtypes: SK, IK and BK channels (small, intermediate and big conductance).

    Small-conductance Ca2+-activated K+ channels (SK channels) underlie the medium duration after hyperpolarization that follows single or trains of action potentials in many types of neurons. This family is composed of KCa2.1 (SK1), -2.2 (SK2), and -2.3 (SK3) isoforms, which are expressed differentially within the central nervous system (CNS)1,2.

    CyPPA is an activator of small conductance KCa channels that displays selectivity for SK2 and SK3 channels (EC50 values are 5.6 and 14 µM for SK3 and SK2 respectively and efficacy is 90% and 71% for hSK3 and hSK2, respectively)3. CyPPA displays no activity at SK1 and IK (KCa3.1) channels3.

    CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels from one another. Therefore, it enriches the repertoire of tools available to test the hypothesis that SK channels may be targets for future CNS drugs4.

    CyPPA was found to block TRPM7 channels, demonstrating an overlap between pharmacological compounds acting on TRP and KCa channels5.

    Target KCa2.2, KCa2.3, TRPM7 channels
    Last update: 24/01/2020

    CyPPA (#C-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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