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
Prazosin (MDCK-II)
Genistein (Caco-2)
CCK-8 (Vesicles)
Subcellular Localization in Assay Model – Apical (in cells)
Inhibition Positive Controls – Ko143 (MDCK-IIA)
Chrysin (Caco-2)
Bromosulfophthalein (Vesicles)