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MDCKII Monolayer Assays

ServiceTransporterTechnologyBarrier
MDCKII-BCRP substrate assessment BCRP
Monolayer Assay
Blood-brain-barrier
Intestinal Barrier
Hepatic Barrier
MDCKII-BCRP inhibitor assessment BCRP
Monolayer Assay
Blood-brain-barrier
Intestinal Barrier
Hepatic Barrier
MDCKII-BCRP DDI - IC50 determination for prazosin inhibition BCRP
Monolayer Assay
Blood-brain-barrier
Intestinal Barrier
Hepatic Barrier
MDCKII-mBcrp1 substrate assessment Bcrp - mouse
Monolayer Assay
Blood-brain-barrier
Intestinal Barrier
Hepatic Barrier
MDCKII-MDR1substrate assessment MDR1/P-gp
Monolayer Assay
Blood-brain-barrier
Hepatic Barrier
Renal Barrier
Intestinal Barrier
MDCKII-MDR1inhibitor assessment MDR1/P-gp
Monolayer Assay
Blood-brain-barrier
Hepatic Barrier
Intestinal Barrier
Renal Barrier
MDCKII-MDR1 DDI - IC50 determination for digoxin inhibition MDR1/P-gp
Monolayer Assay
Blood-brain-barrier
Hepatic Barrier
Intestinal Barrier
Renal Barrier
MDCKII-mBcrp1 inhibitor assessment Bcrp - mouse
Monolayer Assay
Blood-brain-barrier
Intestinal Barrier
Hepatic Barrier
MDCKII-mBcrp1 DDI - IC50 determination for prazosin inhibition Bcrp - mouse
Monolayer Assay
Blood-brain-barrier
Hepatic Barrier
Intestinal Barrier
MDCKII-OATP2B1/BCRP substrate assessment BCRP
OATP2B1
Monolayer Assay
Hepatic Barrier
MDCKII-OATP2B1/BCRP inhibitor assessment BCRP
OATP2B1
Monolayer Assay
Hepatic Barrier
MDCKII-OATP2B1/BCRP DDI - IC50 determination for E3S-inhibition BCRP
OATP2B1
Monolayer Assay
Hepatic Barrier

Description

The introduction of transporter transfected cell lines capable of forming tight cell layers facilitated the investigation of 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.

SOLVO’s single transfectant MDCKII cell lines are excellent tools to investigate specific transporter interactions for medium to high permeability test articles. These 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).

Double transfected cell lines are able to mimic physiologically active vectorial transport processes such as the transport of digestive products across the intestinal epithelium from the luminal to the blood side, and the transport of bile salts and other steroid derivatives from the blood to the biliary side in hepatocytes. SOLVO’s 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 and indirect, inhibitory studies (effect of the test articles on the transport of the reporter substrate is measured).

Studies available:

  • Passive permeability in MDCKII transfectants and parentals (uni- or bidirectional)
  • MDR1 substrate assessment in MDCKII-MDR1 transfectants (using specific MDR1 inhibitors)
  • BCRP substrate assessment in MDCKII-BCRP transfectants (using specific BCRP inhibitors)
  • Inhibitor assessments: Drug-Drug Interaction studies: MDR1 (effect on Digoxin transport) and BCRP (effect on Prazosin transport)

MDCKII monolayer studies can be performed in different setups. SOLVO offers a number of standard setups, which differ in terms of the derivable information and cost. These standard setups serve as starting points to define the optimal final study parameters. All setups contain a standard number of controls (e.g. low permeability, high permeability, transporter function).

Setups available:
1. Basic - Studies at one concentration
2. Extended - Studies at several concentrations, more controls
3. FDA Guidelines - Studies according to FDA draft guidance (2006)

These setups can be customized to suit your needs.

For more information on the MDCKII-monolayer technology background, please click here.