Drug Transporter Inhibition


Sekisui XenoTech's Discovery Plus™ Transporter Inhibition studies provide a first look at the possible interaction between new drug candidates and the transporters listed in the FDA, PMDA and EMA DDI guidance documents. Drug transporters can affect the ADME properties of drugs and have the potential to be involved in drug-drug interactions.

Discovery Plus™ transporter inhibition is a non-GLP service that quickly provides customers with a data summary of results. Our assay designs allow the flexibility to mix and match the number of compounds, transporters and concentrations. All experiments are carried out on cell lines expresing the transporter of interest. This service is best utilized for compounds that are in the early discovery phase / early development phase. For compounds that will be submitted for regulatory agency approval, please utilize our definitive drug transport services.

Discovery Plus™ Transporter Inhibition Overview
  • Incubations performed in 24-well transwell plates (P-gp and BCRP) or 24-well cell culture plates for SLC transporters
  • Incubations performed in triplicate
  • Positive control inhibitors included
Transporter Test System Probe Substrate (µM)
P-gp (MDR1) Caco-2 cells digoxin
BCRP MDCKII-BCRP cells Prazosin
OATP1B1 HEK293 cells 3H-Estradiol-17β-glucuronide
OATP1B3 HEK293 cells 3H-Estradiol-17β-glucuronide
OCT2 HEK293 cells 14C-Metformin
OAT1 HEK293 cells 3H-Estrone-3-sulfate
OAT3 HEK293 cells 3H-Tetraethylammonium bromide

Discovery Plus™ Transporter Inhibition Results
A tabulated summary of the following will be provided:
  • % Inhibition values
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