hERG screening for small molecule inhibitors of hERG.
hERG Membrane Preparation (10 μg/well) was characterized by hERG screening with known hERG blockers 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.


PrecisionION Recombinant hERG Potassium Ion Channel Membrane Preparation
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.
Better hERG Screening
The PrecisION Recombinant hERG Potassium Ion Channel Membrane Preparation enables high-throughput binding assays for rapid, cost-effective hERG screening. Cardiotoxicity caused by hERG potassium channel blockade and can result in the costly withdrawal of drugs or late-stage termination of drug development. Detecting potential cardiotoxicity early can save significant cost and time.

Advantages of PrecisION hERG Membrane Preparations:
How does hERG channel blockage cause cardiotoxicity?
The human ether-à-go-go-related gene (hERG) encodes the potassium ion channel responsible for the delayed rectified potassium current IKr. Several classes of drugs can inhibit IKr, resulting in delayed repolarization (measured as a long QT interval) and possible cardiotoxicity. As a result, the U.S. FDA and ICH S7B guidelines have set out a non-clinical testing strategy to assess the effects of pharmaceuticals on ventricular repolarisation and proarrhythmic risk.

Product Listing: Ion Channel Membrane Preparations