A reversible anion channel blocker against VRAC (VSOAC) and CaCC channel anoctamin (ANO).
NS3728 (Endovion) is a di-aryl-urea-based reversible anion channel blocker that is shown to inhibit Ca(2+)-independent Cl- conductance by volume-regulated anion channel (VRAC or VSOAC; IC50 = 400 nM) as well as Ca2+-activated Cl- ccurrent (CaCC) by anoctamin (ANO) in an apparently voltage-dependent manner (IC50 against ANO1 = 2.1 and 0.7 μM at -95 and +50 mV, respectively). NS3728 is reported to be 5.5-times more potent than Tamoxifen against VRAC (IC50 = 0.4 vs. 2.2 μM).
The Journal of membrane biology, 196(2), 83-94 (2004-01-16)
The endogenous volume-regulated anion channel (VRAC) from HEK293 cells was pharmacologically characterized using the whole-cell patch-clamp technique. Under isotonic conditions a small (1.3 nS), Ca(2+)-independent Cl conductance was measured. However, swelling at 75% tonicity activated a VRAC identified as an
Journal of cellular physiology, 210(3), 831-842 (2006-11-18)
Recent evidence implicates the volume-regulated anion current (VRAC) and other anion currents in control or modulation of cell cycle progression; however, the precise involvement of anion channels in this process is unclear. Here, Cl- currents in Ehrlich Lettre Ascites (ELA)
American journal of physiology. Cell physiology, 310(11), C857-C873 (2016-03-18)
The leucine-rich repeat containing 8A (LRRC8A) protein is an essential component of the volume-sensitive organic anion channel (VSOAC), and using pharmacological anion channel inhibitors (NS3728, DIDS) and LRRC8A siRNA we have investigated its role in development of Cisplatin resistance in
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