PERMEABILITY AND TRANSPORTERS

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