Senicapoc

Senicapoc is an inhibitor of intermediate conductance calcium-activated potassium (IK_Ca1/K_Ca3.1) 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 IK_Ca1/K_Ca3.1 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. Stocker, J.W., De Franceschi, L., McNaughton-Smith, G.A., et al. ICA-17043, a novel gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice. Blood 101(6), 2412-2418 (2003).

2. Staal, R.G.W., Khayrullina, T., Zhang, H., et al. 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. Hansen, L.K., Sevelsted-Møller, L., Rabjerg, M., et al. Expression of T-cell KV1.3 potassium channel correlates with pro-inflammatory cytokines and disease activity in ulcerative colitis. J. Crohns Colitis 8(11), 1378-1391 (2014).