MDCK-MDR1 Permeability Assay
In addition to the permeability of CaCO-2 cells, the MDCK-MDR1 cell permeability test is another test widely used to screen the permeability of compounds. MDCK-MDR1 cells stably transfer and express the MDR1 gene (ABCB1) in MDCK cells, which encodes and expresses the efflux protein P-gp that causes multiple drug resistance.

Like the CaCo-2 cell permeability test, MDCK-MDR permeability analysis calculates the Efflux Ratio by measuring the transport from AB and BA in two different directions, so as to determine whether a molecule has active efflux mediated by P-gp .

MDCK-MDR permeability analysis helps to understand the mechanism of compound efflux, and helps to find problems related to drug permeability in the early development stage.

MDCK-MDR permeability analysis can not only predict the intestinal wall permeability of the compound, but also can be used to predict the ability of the compound to cross the blood-brain barrier.

MDCK-MDR1 Permeability Assay Protocol

Compound required 2mg or 100µL 10mM DMSO solution
Test concentration 10µM
Cell cuture 3 days
Replicates N=2
Incubation Condition Incubation in CO2 incubator at 37ºC for 90 min
P-gp inhibitor Cyclosporin
Integrity of the monolayer TEER>200 Ω•cm2
Analysis method LC-MS/MS
Data delivery Papp, Efflux Ratio, %Recovery
Data Calculation Papp = CRecx VRec/ (A x t x C0)
Efflux Ratio = Papp (B→A) /Papp (A→B)
Recovery = [(Vrec x Crec) + (Vd x Cd)] / (Vd x C0)
Data Interpretation Efflux>2.0 without Pgp inhibitor, P-gp substrate
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