E-4031 acts on a specific class of voltage-gated potassium channels mainly found in the heart, the hERG channels. hERG channels (Kv11.1) mediate the IKr current, which repolarizes the myocardial cells. The hERG channel is encoded by ether-a-go-go related gene (hERG). See more E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. See more E-4031 is a synthesized toxin that is a methanesulfonanilide class III antiarrhythmic drug. See more As E-4031 can prolong the QT-interval, it can cause lethal arrhythmias. See more E-4031 is solely used for research purposes. So far, one clinical trial has been conducted to test the effect of E-4031 on prolongation of the QT-interval. See more E-4031 blocks hERG-type potassium channels by binding to the open channels. Its structural target within the hERG-channel is unclear, but some other methanesulfonanilide class III antiarrhythmic drugs are known to bind to the S6 domain or See more WebApr 24, 2024 · Irradiation (0 and 5 Gy) and post-incubation (8 h) were carried out either in the absence (1 st and 3 rd plot) or presence (2 nd and 4 th plot) of the hERG channel inhibitor E4031 (3 µM).
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WebAn isoleucine mutation in human ether-a-go-go-related gene (hERG) abolishes its interaction with E-4031. E-4031 selectively blocks hERG K + channels. Features and … WebMay 1, 2024 · For both Pluricyte® Cardiomyocytes and GP-CMs the response to the hERG channel blockers was less sensitive than expected based on literature (E4031 hERG … how did ww2 affect japanese americans
E-4031 dihydrochloride Supplier CAS 113559-13-0 - Tocris …
WebApr 1, 2024 · Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37°C with an IC50 of 7 nM, 18 nM, 343 μM, 165 nM, and 214 nM, … WebIC50 values for binding affinity for the hERG K+ channel in a solution of hERG/HEK293 membranes: 49 nm References:-Maris Vilums et al. "Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues" Chem Med Chem 2012, 7, 107–113: Web(IC50). HERG current is measured as the peak outward current during the ramp down phase. To quantify drug potency against hERG channels using this protocol, the steady state hERG current how did world wars i and ii affect germany