Vesicular Transport Assays
Description
The vesicular transport assay is performed using inside out vesicles from membranes expressing the transporter of interest. The method can be applied to measure either inhibitory or substrate type interactions with ABC efflux transporters. The vesicular transport inhibition assay is a robust and quick assay suitable for screening large numbers of compounds. The read-out of the assay is easy to interpret and suitable for IC50 determinations (ITC reference ). The success of substrate assays depends very much on the passive permeability of the compound. High permeability compounds will diffuse out of the vesicles and therefore will not be detected as substrates.
SOLVO Biotechnology offers vesicular transport substrates studies in four levels. The launch of the given Part(s) depend(s) on the success of the previous Part(s).
Part 1 – Vesicular Transport inhibitor assessment (IC50 determination)
Part 2.1. – Vesicular Transport substrate assessment - feasibility studies: pilot experiments to determine the feasibility of testing
Part 2.2. – Vesicular Transport substrate assessment - characterization studies: Detailed characterization of the transport, determination of KM and Vmax
Part 2.3. – Optional Part for characterizing potential drug-drug interactions
Advantages of the Vesicular Transport Assay
Inhibition analysis suitable for any type of compound concerning its permeability
• Uptake measurements for low to medium permeability compounds
• Quick and easy
• Modelling of IC50 concentration
• Vesicles can be prepared from any cell type
• Large dynamic range
• Flexible readout (LSc, Fluo, LC/MS)
Learn more about the Technology background of the Vesicular Transport Assay
For each of the Vesicular Transport Assays listed above characterization files with more information about the performance of the assay are available. Characterization files describe the time-linearity course for a given probe substrate, the concentration dependent kinetics (Km/Vmax) determined and IC50 values generated for selected inhibitors. To request this information please contact your local Business Development representative directly or send a general inquiry to .(JavaScript must be enabled to view this email address).
