Kidney Transporter Assays

The kidney transporter assays provide a means to assess whether a test compound is a potential substrate or inhibitor of specific drug transporters within the kidney. We provide kidney transporter assays for small molecule formulations such as pharmaceuticals, industrial chemicals and consumer products.

Our kidney transporter assays use a novel renal line and genetically modified versions of this created with our proprietary CompoZr® zinc finger nuclease (ZFN) technology.

The kidney is a major site of elimination for many drugs. Much of this renal clearance is mediated by uptake and efflux transporters. Interference with transporter function has been linked to adverse effects due to drug accumulation in proximal tubules and drug-drug interactions. Renal transporter assays may help in the identification of renal excretion or elimination mechanisms and potential drug-drug interactions.

We developed a human proximal tubule epithelial cell line with extended proliferative capacity. These cells have been characterized for proximal tubule cell functions, including numerous uptake and efflux transporters. We have also begun developing a number of transporter knockout cell lines (e.g., MDR1 KO) to use in conjunction with the parental line. These cell lines are suitable for studying the transport properties of test substances in a human proximal tubule cell milieu. 
 

 Kidney Transporter Uptake Assay Protocol

 
Test System RPTECs (Control)
Test Compound Concentration 10 µM, or custom
Replicates 3
Assay Length 10 minutes
Controls Vehicle (0.1% DMSO)
TEA (tetraethylammonium)
PAH (para-aminohippuric acid)
Analysis Method LC/MS
Data Delivery Intracellular accumulation

 

 Kidney Transporter Efflux Assay Protocol

 
Test System RPTEC (Control)
RPTEC, MDR1 KO
Test Compound Concentration 10 µM, or custom
Replicates 3
Assay Length 10 minutes
Controls Vehicle (0.1% DMSO)
Calcein-AM
Analysis Method Fluorescence, LC-MS/MS
Data Delivery Intracellular accumulation

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