Validated in Performance, Accuracy and Quality
In cooperation with Cytocentrics AG CCS has developed a set of recombinant cell lines stably expressing ion channels of high pharmacological relevance.
The cell lines have been generated by stable transfection of HEK293 or CHO-K1 cells and subsequent clonal selection. They have been characterized in manual and automatic patch clamp assays regarding their electrophysiological and pharmacological properties using conventional whole cell recordings.
Cells are supplied either on basis of a licence agreement with the option to propagate the cells in-house or as aliquots of assay-ready frozen cells. Each batch of frozen cells has been validated in patch clamp assay and has a documented assay window and Z'-factor.
- Validated cell line for manual and automatic patch clamp assays.
- Stability of expression tested for 20 passage doublings.
- Stable Giga-Ohm sealing and high peak tail current (>200 pA).
- Robust assay parameters e.g. S/B, Z' and CV.
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hERG HEK293
hERG-HEK293 is a recombinant cell line expressing human ERG (Ether-a-go-go Related Gene) potassium channel KV11.1 which is coordinating the heart's beating. Inhibiton by hERG results in QT prolongation and fatal cardiac arrhytmias. Binding of compounds to hERG may result in abnormal cardiac rhythms. Therefore, all new drug entities have to undergo a cardiotoxicity screening. The hERG-HEK293 cell line is a perfect tool to test compounds for ther cardiac safety .
Fig.1: hERG Currents
Representative hERG outward currents recorded from Instant hERG-HEK293 cells. Currents were elicited upon depolarization of the membrane to +40 mV in 10 mV increments. hERG tail currents were elicited by repolarizing step to -65 mV (2 s).
Fig.2: hERG Blockage
Inhibition of hERG tail currents by different compounds. Tail currents were normalized to the control.
NaV1.5 CHO
NaV1.5-CHO is a recombinant cell line expressing human cardiac sodium channel. NaV1.5 plays a central role in the generation of the cardiac action potential and propagation of electrical impulses in the heart. Inhibition of NaV1.5 results in long QT syndrome type 3 and ventricular fibrillation. Binding of drugs to NaV1.5 may result in abnormal cardiac rhythms. Therefore, NaV1.5 is now being included in cardiotoxicity screening. The NaV1.5-CHO cell line is a perfect tool to test new compounds for their cardiac safety .
Fig.1: NaV1.5 Currents
Representative current traces were recorded from NaV1.5-CHO Instant Cells. Typical currents were evoked by a voltage-step protocol starting from a holding potential of -100 mV in 10 ms pulses to test voltages from -60 to +80 mV in 10 mV increments. The current-voltage relationship of the Instant Cells are virtually identical to that observed with a running cell culture.
Fig.2: NaV1.5 Blockage
Inhibition of NaV1.5 tail currents by different compounds. Tail currents were normalized to the control.