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Currently Available Single Transporter Assay-Ready Plates
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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
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TransFlex Assay Ready Tutorial
Flexible, Assay-Ready Transporter Plates…on Demand
Optivia Biotechnology is pleased to announce the launch of the TransFlex™ transporter assay system. Utilizing the same technology as our Opti™ line of transporter assay services, researchers now have the option of using assay-ready transporter plates expressing a variety of transporters in-house. TransFlex plates 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, or many compounds that you need to test against a single transporter, 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
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.
The following drug transporters are recommended for testing by the FDA, EMA, and PMDA: BCRP, MATE1, MATE2-K, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, and P-gp
Figure 1. signal-to-background activities for the regulatory transporters currently in the TransFlex product line. The substrates used in the assays are as follows (transporter, substrate): OATP1B1, E17bG; OATP1B3, CCK-8; OAT1, PAH; OCT1, MPP+; for OCT2, MATE1, and MATE2-K, metformin is the substrate; P-gp, quinidine; and BCRP, prazosin. For the uptake transporters, the activity is compared to that of the control cells; for the P-gp & BCRP transporters, the efflux activity (B>A transport) is compared to A>B transport.
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.