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Ion Channels in Drug Discovery and Safety Pharmacology

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Ion channels are well known for regulating electrical activity in excitable cells, and many roles in non-excitable tissues continue to be uncovered. They are important therapeutic targets in a range of indications including arrhythmia, hypertension, local anesthesia, pain, stroke, epilepsy, depression, bipolar disorder, COPD, autoimmune disorders and diabetes. Not only are ion channels important drug targets, but they are also generally relevant for drug safety. Indeed, many drugs withdrawn from the market due to cardiac related adverse effects have been shown to block the human ether-a-go-go (hERG) ion channel, which delays repolarization of the cardiac action potential and can result in a potentially fatal arrhythmia known as Torsades de Pointes (TdP).

Through the combined expertise of Cerep, Panlabs, and IonChannelProfiler™ services, Eurofins offers a broad portfolio of both binding and functional assays for ion channels. Our years of experience as an ion channel CRO has enabled us to better understand our customers' latent needs, so if you're looking for an ion channel screening solution, you've found it.

   

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Advantages of Ion Channel Profiling with Eurofins:

  • Robust binding and functional cell based assays performed with stability-tested PrecisION® cell lines
  • Assays for agonist, antagonist, NAM and PAM activity
  • Over 9 years of experience and the first CRO to provided testing by automated electrophysiology in 2005
  • Only CRO in the industry that offers services on IonFlux HT™
  • Over 60 ion channel targets and >130 assays available on Manual Patch Clamp, IonWorks®, PatchXpress®, IonFlux HT™ QPatch® systems
  • Quick turnaround times of 2-3 weeks depending on project type
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Figure 1. IonChannelProfiler™ services can generate quality hERG data with higher throughput using the IonWorks® platform.

Correlation between IonWorks® IC50 values using PrecisION® hERG stable cell lines (Cat. No. CYL3038) and published values obtained using manual patch clamp for seven reference compounds. Most fall on the line of equivalence (shown in black), or within a 3-fold range of this (light blue lines), indicating good correlation between methodologies.

(*Services mentioned in report for Cerep, EMD Millipore and Ricerca Biosciences are now operated by Eurofins)