Cayman DCPIB

DCPIB is an inhibitor of volume-regulated anion channels (VRAC).¹ It inhibits the swelling-induced chloride current (I_Cl,swell) in bovine pulmonary artery endothelial cells (IC₅₀ = 4.1 µM). DCPIB inhibits the VRAC subunit leucine-rich containing 8A (LRRC8A; IC₅₀ = 20.9 µM) and inhibits sphingosine-1-phosphate-induced cGAMP uptake by LRRC8A in telomerase-immortalized human microvascular endothelial (TIME) cells when used at a concentration of 20 µM.^2,3 It also inhibits the two-pore domain potassium channels K_2P18.1/TRESK, K_2P3.1/TASK1, and K_2P9.1/TASK3 in COS-7 cells expressing the human channels (IC₅₀s = 0.14, 0.95, and 50.72 µM, respectively).⁴ DCPIB (10 µM) activates K_2P2.1/TREK1 and K_2P4.1/TRAAK channels in COS-7 cells expressing the human channels. Intracisternal administration of DCPIB (20 µg/kg) reduces infarct area and neurological deficit scores in a rat model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO).⁵

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