Key result
The 293B-related substance IKs124 blocked hKCNE2/hKCNQ1 channels with an IC50 of 8 nM, suggesting potential as a subunit-specific blocker for peptic ulcers.
Population
COS cells and mouse parietal cells
Design
Preclinical
Authors
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IKs124 may target parietal cell K+ channels for peptic ulcers; hypothesis-generating in animal models and leaves open human translation.
Effect estimate: IC50 8 nM
KCNQ1 coassembles with KCNE2 to form acid-activated luminal K+ channels in parietal cells, which can be potently blocked by IKs124, suggesting a potential target for peptic ulcer treatment.
Heitzmann et al. (2004) studied this question. IKs124 was evaluated on Inhibition of hKCNE2/hKCNQ1 channels (IC50 8 nM). The 293B-related substance IKs124 blocked hKCNE2/hKCNQ1 channels with an IC50 of 8 nM, suggesting potential as a subunit-specific blocker for peptic ulcers.
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