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MTOX1021 Sigma-Aldrich

HepaRG Cells BCRP (-/-)

one vial



Related Categories ADME/Tox Products, Cell Biology, Cell Line Models, Liver Drug Transporter/Toxicity Models
Quality Level   200
biological source   human female liver (hepatocarcinoma and hepatitis C tumor)
OMIM accession no.   603756
storage temp.   −196°C
Gene Information   human ... ABCG2(9429)


General description

HepaRG is a human hepatoma cell line. The cells possess a pseudodiploid karyotype and have been characterized as an oval ductular bipotent hepatic cell line as they have the ability to differentiate into both biliary and hepatocyte lineages in the presence of DMSO. HepaRG BCRP knockout cells express the major xenobiotic sensors (PXR, CAR and AhR), drug transporters, phase I and II drug metabolizing enzymes as well as key hepatic transcription factors involved in stress response pathways.


See technical bulletin for detailed protocols

Features and Benefits

HepaRGcells are the most metabolically active human hepatocyte cell line developed to date. These the cells are suitable for a wide variety of studies for drug metabolism, CYP induction, metabolism-mediated toxicity, transporter, and hepatotoxicity. - Sigma′s HepaRG BCRP Knockout (KO) allows investigations of drug-transporter interactions involving BCRP in the liver.

Zinc finger nucleases (ZFN) mediated Knockout of ABCG2 (BCRP) gene.
• The frame-shift mutation of ABCG2 gene was confirmed by fragment length analysis and DNA sequencing.
• Loss of functionality was confirmed by loss of transport of selective substrates in sandwich culture assay.


Tested for Mycoplasma, sterility, post-freeze viability, short terminal repeat (STR) analysis for cell line identification, cytochrome oxidase I (COI) analysis for cell line species confirmation.

Legal Information

Exhibit 1: ADME/Tox cell lines license
Exhibit 2: HepaRG limited use license

HepaRG is a trademark of BioPredic International company

Safety & Documentation

Safety Information

UN 3245 9
WGK Germany 
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable


Certificate of Analysis (COA)

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Protocols & Articles


The Role of Liver Transporters in Drug-Drug Interactions

Oral drug delivery involves dissolution in the small intestine and absorption across the enterocyte barrier into the portal vein followed by subsequent delivery through the liver into the systemic ci...
David C. Thompson, Ph.D, R&D Manager, Sigma® Life Science and Michael D. Mitchell, Product Manager, Sigma® Life Science
Biofiles Vol. 8, No. 12
Keywords: Absorption, Cancer, Clinical, Eliminations, Genetic, Metabolic Pathways, Metabolism, Pharmaceutical, Polymorphisms

Peer-Reviewed Papers


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