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Ion Channel Screening Cell Lines

Ion Channel Screening Cell Lines

Aurora Biomed offers purchasing and licensing of cell lines for some of the most common drug discovery ion channel targets. The cell line collection includes stably expressed hERG potassium channels, Kv1.3 potassium channels, or Nav1.5 sodium channels, each optimized and validated using both flux assays and electrophysiology. The window of detection (signal/noise) of these cell lines is appropriate for high-throughput screens. Use with Aurora Biomed’s Ion Channel Reader Series and optimized reagents, can generate robust, sensitive assays for ion channel screening.

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hERG Cell Line

Drug-induced blockage of the human ether-a-go-go (hERG) potassium channel is associated with prolonged QT, which can predispose individuals to arrhythmias such as Torsades de Pointes. Therefore, early screening of compounds for hERG channel activity is a vital step in the drug-discovery process. Our CHO-hERG cell line was developed and validated as a tool for screening compounds which may lead to QT prolongation. These cells:

  • Stably express hERG potassium channels
  • Have been validated using electrophysiology and flux assay
  • Are suitable for high-throughput screening(HTS)

Kv1.3 Potassium Channel Cell Line

The Kv1.3 potassium channel has shown promise as a pharmaceutical target for such diseases as multiple sclerosis, obesity, and more recently, diabetes. In order to screen large compound libraries against Kv1.3, a reliable expression system is needed. Aurora’s CHO-Kv1.3 potassium channel cell line is designed to express high levels of Kv1.3 channels, and to show uniform expression over time. These cells:

  • Stably express Kv1.3 potassium channels
  • Have been validated using electrophysiology and efflux assay
  • Are suitable for high-throughput screening (HTS)

Publications:

High-Throughput Screening for Kv1.3 Channel Blockers Using an Improved FLIPR-Based Membrane-Potential Assay

Nav1.5 Sodium Channel Cell Line

The cardiac sodium channel Nav1.5, also known as hH1a, is an important target for cardiotoxicity screening as mutations in its gene (SCN5a), contribute to a type of long-QT syndrome (LQT3). Abnormal heart rhythms due to this mutation are more likely to be fatal than those due to LQT1 (KVLQT1) or LQT2 (hERG). Moreover, it is a well known fact that non-specific binding of drugs with this channel may lead to abnormal cardiac arrhythmias. Therefore, Nav1.5 is now included in cardiotoxicity screening panels. Early screening of novel chemical entities (NCEs) for Nav1.5 channel activity is a vital step in the drug-discovery process. Our HEK-Nav1.5 sodium channel cell line was developed and validated as a tool for screening such NCEs. This sodium channel cell line:

  • Stably express cDNA of Nav1.5 sodium channel
  • Have been validated using electrophysiology and flux assay
  • Are suitable for high-throughput screening (HTS)
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