PrecisION Recombinant hERG Potassium Ion Channel Membrane Preparation
FDA, ICH S7B guidelines set out a non-clinical testing strategy to assess the effects of pharmaceuticals on ventricular repolarisation and proarrhythmic risk. The most common mechanism for this is inhibition of the delayed rectified potassium current IKr. The human ether-à-go-go-related gene (hERG) encodes the potassium ion channel responsible for IKr.
Several classes of drugs produce life-threatening cardiac toxicity associated with the prolongation of the long QT interval. This toxicity is caused by hERG K+ channel blockade and can result in the costly withdrawal of drugs or late stage termination of drug development. The early detection of potential cardiotoxicity can yield significant cost and time savings. A high-throughput binding assay will rapidly and cost-effectively identify compounds that interact with the hERG channel.
To complement our functional assays, Millipore provides membranes for hERG radioligand binding assays. These have been validated using several different radioligands and provide comparable data to that found in the literature. While not providing a functional measure of hERG activity, the very high throughput of radioligand binding assays have made this a very useful approach for monitoring potential hERG liability at the earliest phase of drug discovery. Here, the primary aims are to raise flags which could trigger follow-up studies, such as electrophysiological screening.
Rank ordering small molecule inhibitors for hERG. hERG Membrane Preparation (10 μg/well) was characterized by evaluating the activity for known hERG small molecule inhibitors in a competition binding assay. The membranes were incubated with 3.0 nM [3H]-Astemizole and increasing concentrations of unlabeled compounds to determine sample activity and rank order.
Advantages of Millipore hERG Membrane Preparations
- High functional expression and specific binding
- Created from stable cell lines for consistent performance
- Validated using three different radioligands (Astemizole, Dofetilide, BeKm-1
- Available in bulk quantities
Product Listing
| CYL4039 | hERG | human | HEK |
Nouveaux produits et nouvelles publications
- As GPCR Space Becomes More Crowded, Drug Makers Show Affinity for Non-traditional GPCR Binding Sites
- Millipore Corporation and CXR Biosciences Introduce Toxicity Reporter Assay Panel
- Millipore Launches MILLIPLEX™ MAP
- Millipore Announces Stem Cell Tested Initiative
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