Senicapoc is a potent and selective blocker of the Gardos channel, also known as the Ca2+-activated K+ channel or KCa3.1, with an IC50 of 11 nM. It functions by inhibiting red blood cell dehydration and preventing the increase in cellular hemoglobin concentration, thus having significant implications for various conditions.
- Blocks Ca2+-induced rubidium flux from human red blood cells.
- Inhibits red blood cell dehydration with an IC50 of 30 nM.
- Prevents sickled red blood cell dehydration, a key issue in sickle cell disease.
- Reduces airway hyperresponsiveness and eosinophil numbers in asthma models.
- Demonstrated potential applications in acute respiratory distress syndrome, COVID, dehydrated hereditary stomatocytosis, mild cognitive impairment, Alzheimer's disease, and pulmonary fibrosis.