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Novel intramolecular photoinduced electron transfer-based probe for the Human Ether-a-go-go-Related Gene (hERG) potassium channel.

Analyst. 2015; 
LiuZhenzhen,ZhouYubin,DuLupei,LiMin
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Cellular Analysis … folds, 6-8 points) when applied to the binding assays Cell membranes were prepared following the manufacturer's instructions described by GenScript USA Inc (Cat No # M00355) First, each well of Uni-filter 96 GF/C microplate … Get A Quote

摘要

Drug induced long QT syndrome is a high risk event in clinic, which mainly results from their high affinity to the Human Ether-a-go-go-Related Gene (hERG) potassium channel. Therefore, evaluation of the drug's inhibitory activity against the hERG potassium channel is a required step in drug discovery and development. In this study, we developed a series of novel conformation-mediated intramolecular photoinduced electron transfer fluorogenic probes for the hERG potassium channel. After careful evaluation, probes N4 and N6 showed good activity and may have a promising application in the cell-based hERG potassium channel inhibitory activity assay, as well as potential hERG-associated cardiotoxicity evalu... More

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