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DCEBIO is an activator of intermediate conductance calcium-activated potassium (IKCa1/KCa3.1) channels and a dichlorinated derivative of the KCa channel activator 1-EBIO (Item No. 14575).1 It activates IKCa1/KCa3.1 and induces chloride secretion in T84 monolayers in a concentration-dependent manner, an effect that can be blocked by the IKCa1 inhibitor charybdotoxin (Item No. 24115). DCEBIO potentiates the activity of small conductance calcium-activated potassium (SK) channels with an EC50 value of 27 µM in HEK293 cells expressing recombinant human SK2 channels by increasing the apparent calcium sensitivity of the channel.2 It also potentiates SK channel-mediated apamin-sensitive after-hyperpolarizing currents (IAHP) in CA1 pyramidal neurons, increasing the amplitude and duration of IAHP when used at a concentration of 100 µM. DCEBIO induces chloride secretion in isolated mouse jejunum (EC50 = 41 µM), an effect that is reduced by the cystic fibrosis transmembrane conductance regulator (CFTR) inhibitors glibenclamide and NPPB.3
WARNING This product is not for human or veterinary use.
1. Benzimidazolone activators of chloride secretion: Potential therapeutics for cystic fibrosis and chronic obstructive pulmonary disease. J. Pharmacol. Exp. Ther. 296(2), 600-611 (2001).
2. Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current IAHP and modulates the firing properties of hippocampal pyramidal neurons. The Journal of Biological Chemisty 280(50), 41404-41411 (2005).
3. DCEBIO stimulates Cl-