TransFlex™ Multi-Transporter Model Plates

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TransFlex™ Multi-Transporter Model Plates

Currently Available Multi-Transporter Model Assay-Ready Plates

  • OCT2 + MATE1
  • OCT2 + MATE2-K
  • OCT2 + MATE1 + MATE2-K
  • OATP1B1 + BCRP
  • OATP1B1 + MRP2
  • OATP1B3 + BCRP
  • NTCP + BSEP
  • OATP1B1 + NTCP + BSEP
  • OATP1A2 + MDR1 + BCRP

CONTACT US TO LEARN MORE

TransFlex Assay Ready Tutorial

Flexible, Assay-Ready Plates…on Demand

Generate more insightful data with these indispensable assays

TransFlex Multi-transporter model, assay-ready plates are now available! Designed for mechanistic studies of drug clearance and tissue exposure, Optivia’s unique multi-transporter models consist of polarized MDCK-II cells expressing various combinations of uptake and/or efflux transporters. These assays help to reproduce the synergistic effects these transporter combinations have on drug disposition in the liver, kidney and BBB. Now available in our TransFlex 96-well, assay-ready plate format, these state-of-the art mechanistic models allow you to start generating more insightful data 24 hours after they arrive at your facility. These assays:

  • Provide mechanistic models for liver, kidney and BBB transporters
  • Allow evaluation of drug clearance and tissue exposure—simultaneously
  • Simplify the study of low-permeability compounds as efflux transporter substrates

Produced using the same Opti-Expression™ technology proven by our trusted transporter assay services, TransFlex assay-ready plates provide a convenient way to perform single and multi-transporter assays in house: they require minimal cell culture and maintenance, and plate formats can be customized to an assortment of configurations. Whether you have a single compound that you need to test against a variety of transporters, many compounds that you need to test against a single transporter, or one or more compounds that you need to test in a multi-transporter model system, we can design plates to suit your needs.

  • Ready to use 24 hours after receipt
  • Suitable for both substrate and inhibition studies
  • Available for a variety of single-transporter and multi-transporter models
  • Easy to use 96-well format
  • Flexible plate configurations allow multiple transporter options plus control cells on the same plate
  • No costly cell line development or maintenance

Flexible Transporter Assay Configurations

oct2_m1-models-b_a-90min

Comparison of the effects of different transporters on cellular accumulation of metformin. The data was obtained from a single TransFlex plate containing MDCK-II cells expressing OCT2 (blue) or MATE1 (purple), or OCT2 and MATE1 (green). GFP (white) was used as a control.
Figure 1. Comparison of the effects of different transporters on the transcellular transport (top panel) and cellular accumulation (bottom panel) of metformin. The data was obtained from a single TransFlex plate containing MDCK-II cells expressing OCT2 (blue) or MATE1 (purple), or OCT2 and MATE1 (green).  GFP (white) was used as a control.
 
Sample of multi-transporter plate configurations.
Figure 2. Sample plate configurations for TransFlex multi-transporter models.

Regulatory Transporters Currently Available

Transporters expressed throughout the body affect the plasma and tissue concentrations of a variety of drugs. In particular, uptake and efflux transporters expressed in the intestine, liver, and kidney have been implicated in a variety of serious drug-drug interactions (DDIs). The US FDA, European Medicines Agency (EMA) and Japanese Pharmaceuticals and Medical Devices Agency (PMDA) request that in vitro studies be conducted on nine specific transporters for DDI assessment and drug labeling. Each of these drug regulatory agencies has published DDI guidance documents that differ slightly in the transporters they recommend be tested, in vitro study design, and data interpretation. The TransFlex product line includes transporters recommended by these regulatory agencies. TransFlex regulatory transporter plates allow you to perform your own drug interaction studies on new molecular entities (NMEs) for new drug applications (NDAs), or easily identify potentially safe/unsafe lead compounds early in the drug discovery and development process.

Opti-Expression Technology Platform

TransFlex plates are produced using Optivia’s patented Opti-Expression technology: an in situ transfection method in which cell monolayers are first established and then transfected, without disruption of tight junctions. This method allows the use of control cells consisting of the same parental stock (and having the same passage number) as the experimental cells. In order to ensure the experimental and control cells are treated identically, the control cells undergo control transfections, in which they are transfected with a vector expressing green fluorescent protein (GFP) instead of the transporter being tested. This approach prevents unwanted differences between experimental and control cells—such as variations in passive permeability or flux from interfering endogenous transporters—and avoids the decreased expression of exogenous protein that often plagues ‘stable’ cell lines with increasing passage number. Overall, the approach provides excellent assay reproducibility. For more information about Opti-Expression or the cell lines used, please contact us.