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Senicapoc is an inhibitor of intermediate conductance calcium-activated potassium (IKCa1/KCa3.1) channels.1,2 It inhibits rubidium efflux from and dehydration of isolated human red blood cells (RBCs) induced by the calcium ionophore A23187 (Item No. 11016; IC50s = 11 and 30 nM, respectively).1 Senicapoc (10 mg/kg twice per day) reduces IKCa1/KCa3.1 channel activity, increases potassium levels in RBCs, and decreases erythrocyte density in the SAD transgenic mouse model of sickle cell disease. It inhibits IL-2, IFN-γ, IL-12, and IL-17A production in CD3+ T cells stimulated with phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) and ionomycin (Item Nos. 10004974 | 11932) when used at a concentration of 1 μM.3 Senicapoc (100 mg/kg) increases the paw withdrawal threshold in a rat model of chronic constriction injury (CCI) of the sciatic nerve.2
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1. ICA-
2. Inhibition of the potassium channel KCa 3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury. Eur. J. Pharmacol. 795, 1-7 (2017).
3. Expression of T-