BCRP Transporter Assay (ABCG2)

The BCRP transporter is an efflux transporter that is encoded by the ABCG2 gene. BCRP is also known as Breast Cancer Resistance Protein. BCRP is expressed in many tissues of the body including the apical side of the intestinal lumen, the apical side of the bile canaliculus in liver hepatocytes, and the apical side of the capillaries in the blood brain barrier (BBB). BCRP serves to limit the absorption of substrates, protect them from entering the brain and also to mediate their hepatic elimination.

Optivia offers BCRP substrate and inhibition assays for transport in polarized mammalian cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for BCRP inhibitors as well as Vmax and Km values for BCRP substrates.

BCRP Transporter Relevance Gene Transporter Type Assay Type Species Subcellular Localization in Assay Model Number of Transporters Cell Model Exactly Matched Control Cells Probe Substrate Inhibition Positive Control
FDA & EMA DDI guidances; intestinal and BBB efflux, biliary secretion, renal tubular secretion and drug resistance ABCG2 Efflux Bi-directional Human Apical Selected clone with high BCRP expression Caco-2 clone No Genistein Chrysin
Vesicular accumulation Human, rat N/A Single Vesicle Yes CCK-8 Bromosulfophthalein
Bi-directional Human Apical Single MDCK-II Optional Prazosin KO143