cav1.2 Archives - Sophion

Cav1.2 ready to use cells without rundown

Get your experiments up and running in a matter of few minutes – and maintain the current level for endless minutes, even if the target is the notorious run-down prone Cav1.2. Indeed very convenient to work with these cells provided by NMI TT Pharmaservices. Pharmacology behaves as expected and you can even look for subtle, holding-potential-dependent, differences in state-dependent mode of action. See the whole application report here.

Cav1.2 on QPatch with no rundown

CaV1.2 is widely expressed in the smooth muscle, pancreatic cells, fibroblasts, and neurons. However, it is particularly important and well known for its expression in the heart where it mediates L-type currents, which causes calcium-induced calcium release. It depolarizes at -30mV and is key in defining the shape of the action potential in cardiac and smooth muscle. It is, therefore, a key ion channel for accessing cardiac safety in drug discovery and one of the key channels investigated as a part of the HESI/FDA supported CiPA studies.

When testing compounds on CaV1.2 on the QPatch, we regularly achieve success rates of >85%, however rundown can be high in some CaV1.2 assays, something that makes it inherently difficult. We tested a new CaV1.2 cell line from Charles River Laboratories with very good results. Using this new cell line on the QPatch, you can look forward to rundown rates as low as -1.2% ± 0.6% per minute (n=43), resulting in trustworthy and reliable pharmacology.

You can read more about CaV1.2 assay on Qube 384 and QPatch here.

If you have issues with rundown in your CaV1.2 assay or would like more information and data about this particular cell line contact our application scientists Melanie Schupp.

Cav1.2 on Qube, no rundown

High success rates and minimal rundown with pharmacology according to literature values. The third CaV1.2 cell line, this time kindly provided by Charles River, helps demonstrate how Ca-currents can be recorded stably on automated patch clamp. So, whether you want to investigate the CiPA protocol, interrogate for state dependent mode of action or biophysical characteristics, Qube is the enabling technology. See the full report here.

hCav1.2 recordings on Qube 384 using step, train and CiPA protocols

Some ion channels have a tendency to exhibit reducing current level in the course of an experiment. A notable member of this class is the CaV1.2 channel, a very important ion channel expressed in nervous tissue, the heart and smooth muscle and thus a target for a range of therapeutics as well as a liability target for other groups of medications. Therefore it is important to be able to record reliably, stably and with a high success rate in the pursue of novel compounds with the desired profile on CaV1.2 modulation. Qube 384 provides a stable assay with the CaV1.2 channel generated by SB Drug Discovery with these characteristics:

  • Pharmacology and current-voltage relationship in accordance with literature values
  • Success rates up to 94%
  • Stable currents with rundown as low as (1.2 ± 0.9)% per minute
  • The CiPA protocol yields stable currents with rundown as low as (1 ± 1)% per minute

For the full application report please see here.

Note that we have another Qube Application Report on Cav1.2 on another commercially available cell line underlining the robustness of the Qube platform. Find both of them here

For more information please contact