IndraLab

Statements


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"Vandetanib inhibited WT-hERG current by approximately 86.4 +/- 7.3% (XREF_FIG)."

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"Vandetanib at concentrations of 0.3, 1, and 3 muM reduced I hERG current amplitude by 17.04, 45.32, and 76.05%, respectively (n = 4; XREF_FIG)."

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"Therefore, we speculated that the combination of Gin Rg3 and vandetanib could reverse vandetanib-induced hERG current inhibition and then alleviated the prolongation of QT interval induced by vandetanib."

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"Studies have reported that vandetanib can prolong hiPSC-CM action potential and inhibit hERG current, as well as inhibit both sodium current and calcium current [22]."

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"84 Vandetanib inhibits hERG/KCNH2 channels decreasing IKr current amplitude, leading to a long QT."

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"Furthermore, ginsenoside Rg3 alleviated vandetanib-induced hERG current inhibition and accelerated the process of the channel activation."

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"The results showed that vandetanib exerts blocking effects on both the opening and closing states of hERG channels.The time-dependent effect of vandetanib on hERG channel blocking was produced by the whole-cell patch-clamp technique."

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"Patch-clamp recordings revealed significant reductions of hERG current densities by nilotinib or vandetanib after chronic incubation with hERG-HEK293 cells in addition to the acute inhibition ."

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"Downregulation of hERG Channel Expression By Tyrosine Kinase Inhibitors Nilotinib And Vandetanib Predominantly Contributes To Arrhythmogenesis ."

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"Western blot analysis showed that nilotinib and vandetanib decreased mature hERG protein (155-kDa) expression, in a greater extent than that of the immature form (135-kDa)."

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"In stable transfected human hERG gene HEK293 cells, vandetanib caused concentrate-dependent inhibition in the step and tail currents of hERG."

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"However, the dynamic characteristics of hERG channel current were not studied, and the specific mechanism of prolongation of action potential was not clear.In this study, we analyzed the hERG current dynamic characteristics of vandetanib and found that vandetanib concentration-dependent inhibited the activation of hERG current and the end current of depolarization."

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"Lee et al. [22] found that vandetanib inhibited hERG current, I and I ."

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"Purkinje fiber assays and ion channel studies showed that vandetanib at concentrations of 1 and 3 muM inhibited the hERG currents and prolonged the action potential duration."

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"For example , pre-clinical studies reveal that vandetanib causes hERG block at low concentrations and is associated with both AP prolongation in cardiac tissue preparation and QTc prolongation in vivo suggesting a classical drug-channel interaction [ 226 ] ."

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"The Time Dependence of Gin Rg3 on Vandetanib-Induced hERG Channel Blocking."