P-gp (MDR1) Transporter Assay (ABCB1)

P-glycoprotein (P-gp) is an efflux transporter encoded by the ABCB1 gene; it is also known as Multi-Drug Resistance transporter 1 (MDR1). P-gp (MDR1) is expressed in many tissues of the body, including the kidney, the apical side of the intestinal lumen, the apical side of the bile canaliculus in liver hepatocytes, the apical membrane of proximal tubule epithelial cells, and the apical side of the capillaries in the blood brain barrier (BBB). P-gp (MDR1) limits the absorption of substrates, prevents toxic substances from entering the brain, and is involved in the renal and hepatic elimination of compounds and their metabolites.

BioIVT offers P-gp (MDR1) substrate and inhibition assays for transport in polarized mammalian cells. We offer a wide range of studies, from single concentration screens to full kinetic studies for IC50 determinations for P-gp (MDR1) inhibitors, as well as Vmax and Km studies for P-gp (MDR1) substrates.

 

P-gp (MDR1) Transporter Assay Details
Relevance – FDA & EMA DDI guidances; intestinal and BBB efflux, biliary secretion, renal tubular secretion, drug resistance
Single or Multi-Transporter Model – Single
Transporter Type – Efflux Cell Model – MDCK-II, Caco-2
Assay Type – Bi-directional Exactly Matched Control Cells– N/A
Species – Human Probe Substrate – Quinidine
Subcellular Localization in Assay Model – Apical Inhibition Positive Control – Elacridar