MDCKII Monolayer assays

The introduction of transporter transfected cell lines capable of forming tight cell layers brought the possibility of investigating single transporter interactions on monolayers. MDCKII (Madin-Darby canine kidney strain II cells) cell lines have been widely used as hosts for single and/or double transfections. The difference between efflux ratios on the transfected and parental cell lines is regarded as a sign of transporter mediated active uptake or efflux process.

Single transfectant cell lines

SOLVO's single transfectant MDCKII cell lines are excellent tools to investigate specific transporter interactions for medium to high permeability test articles. These PrediScreen service assays are offered in two modes, direct and indirect setups (effect of the test articles on the transport of the reporter substrate is measured).

Availability

MDCKII-MDR1 Monolayer


Studies

Standard setups


Basic
Studies at one concentration, two time points

Extended
Studies at several concentrations, more time points, more controls

FDA compliant
Studies according to the 2006 FDA Draft Guidance



Substrate assessment: Specific transporter studies



Inibitor assessment: Drug-Drug Interaction studies


IC50 determination for digoxin inhibition

positive control: PSC 833

 



Additional Single Transfectant MDCKII Monolayers

Cell line

Application

Positive control

Negative control

MDCKII-BCRP

Substrate assessment: Direct BCRP interaction, uni- and bidirectional permeability

Transport of prazosin

Parental cell line

Inhibitor assessment: Inhibition of prazosin transport

Ko134

 NA

MDCKII-mBcrp1

Substrate assessment: Direct mBcrp1 interaction, uni- and bidirectional permeability

Transport of prazosin

Parental cell line

Inhibitor assessment: Inhibition of prazosin transport

Ko134

 NA

LLC-PK1-MDR1

under development


Double transfectant cell lines

Double transfected cell lines are able to mimic physiological active vectorial transport processes such as transport of digestive products across the intestinal epithelium from the luminal to the blood side, transport of bile salts and other steroid derivatives from the blood to the biliary side in hepatocytes. PrediScreen double transfected cell line based monolayer studies include the corresponding two single transfectants and the parental cell lines as controls. Double transfected monolayers are suitable for performing both direct, vectorial transport studies as well as indirect, inhibitory studies (effect of the test articles on the transport of the reporter substrate is measured).

Availability

Double Transfectant MDCKII Monolayers

Cell line

Application

Positive control

Negative control

MDCKII-OATP2B1/BCRP

Substrate assessment: Direct vectorial transport

Transport of Estrone-3-Sulfate

Parental cell line and BCRP, OATP2B1 single transfectants

Inhibitor assessment: Inhibition of Estrone-3-Sulfate transport

Estrone and Ko134

 NA

MDCKII-NTCP/BSEP

under development

For more details on the MDCKII Monolayer assays please click here.

This page contains information about following topics: MDCKII cell line,Monolayer assay,Single transfected,Double transfected,Single transfectant cell line,Double transfectant cell line,Definitive assay,MDCK,MCRKII-BCRP,MCRKII-MDR1,LLC-PK,FDA compliant study,Digoxin assessment, Verapamil, Transporter drug-drug interaction, Transporter Oral bioavailability, BBB penetration, Transporter CNS.