Permeability property of a compound greatly affects its oral bioavailability. Caco-2 and MDCK are good models to study permeability and drug transporter interactions. Assessment of drug-transporter interactions helps in the planning of clinical DDI studies.
Drug transporters belong to three categories of transport proteins: ATP-binding cassette (ABC) transporters, solute carriers (SLC) and P-type ATPases.
At Cytovier, we provide Caco-2 and a panel of MDCK-Transporter assays. We offer transporter profiling services to help you select drug candidates with desirable transporter-interaction profiles. Drug transporter assays currently available includes MDR1 (P-gp), BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, BSEP, MATE1, MATE2K, MRP1, MRP2 and MRP4.
Permeability Assay Protocol:
Method: Bi directional
Test article concentration: 1 or 10 µM (other upon request)
Incubation time: 90 minutes
Incubation temperature: 37 C
Number of Replicates: n = 2
Assay condition: HBSS buffer - pH7.4 (other pH upon request)
Cell lines: Caco-2 (20 day culture); MDCK- WT or Transporter transfected
Positive controls: Atenolol, propranolol. Other controls as per transporter
Integrity control: Lucifer Yellow
Analysis Method: LC/MS/MS
Data Delivery: Papp ATOB, BTOA; Efflux ratio; Net efflux where appropriate