BCRP (ABCG2) Transporter Assay
The breast cancer resistance protein (BCRP) is an efflux transporter that is encoded by the ABCG2 gene. BCRP is expressed in many tissues, including the apical side of the intestinal lumen, the apical side of the bile canaliculus in hepatocytes, and the apical side of the capillaries in the blood brain barrier (BBB). BCRP limits the absorption of substrates, prevents toxic substances from entering the brain, and is involved in the hepatic elimination of compounds and their metabolites.
BioIVT offers BCRP 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 BCRP inhibitors, as well as Vmax and Km studies for BCRP substrates.
BCRP Transporter Assay Details
|Relevance – FDA & EMA DDI guidances; intestinal and BBB efflux, biliary secretion, renal tubular secretion and drug resistance
||Single or Multi-Transporter Model – Single|
|Transporter Type – Efflux||Cell Model – MDCK-II, Caco-2, and Vesicle
|Assay Type – Bi-directional in cells; vesicular accumulation in vesicles
||Exactly Matched Control Cells– Yes (MDCK-II only)
|Species – Human||Probe Substrates –
|Subcellular Localization in Assay Model – Apical (in cells)
||Inhibition Positive Controls – Ko143 (MDCK-IIA)