CyPPA. Selective and Potent Opener of KCa2.2 and KCa2.3 Channels
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.
CyPPA is an activator of small conductance Ca2+-activated K+ 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). CyPPA displays no activity at SK1 and IK (KCa3.1) channels. CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels. Therefore, it enriches the repertoire of tools available to test the hypothesis that SK channels may be targets for future CNS drugs.
Alomone Labs is pleased to offer CyPPA (#C-110).
Ion Channel Modulators; K+ Channel Openers
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