Senicapoc

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of the calcium-activated potassium channel KCa3.1 (Gardos channel; KCNN4; IK-1; SK4), with potential anti-inflammatory and immunomodulatory activities. Upon oral administration, senicapoc targets, binds to and inhibits KCa3.1. KCa3.1 regulates membrane potential and calcium signaling in a variety of cells including erythrocytes, activated T and B cells, macrophages, microglia, vascular endothelium, epithelia, and proliferating vascular smooth muscle cells and fibroblasts. The inhibition of KCa3.1 may prevent erythrocyte dehydration in sickle cell disease, reduce fluid secretion, fluid retention and inflammation in the lungs in acute respiratory distress syndrome (ARDS), and reduce inflammation and immune responses in various other diseases such as neuroinflammation in Alzheimer's disease. Senicapoc exhibits good brain penetration.

**Synonyms:** - ICA-17043 - PF-05416266 - SENICAPOC