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MTOX1018

Sigma-Aldrich

BSEP Knockout HepaRG™ Cells

1 vial

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About This Item

UNSPSC Code:
12352207
NACRES:
NA.81

biological source

human female liver (Source Disease: Hepatocarcinoma and Hepatitis C)

form

liquid

storage temp.

−196°C

Gene Information

human ... ABCB11(1351619)

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 BSEP 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.

Application

See technical bulletin for detailed protocols

Features and Benefits

HepaRG cells 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, cholestasis, and hepatotoxicity.

  • Sigma′s HepaRG BSEP Knockout (KO) allows investigations of drug-transporter interactions and bile acid biosynthesis, accumulation (Cholestasis), and transport involving BSEP in the liver.

Zinc finger nucleases (ZFN) mediated Knock-out of ABCB11 (BSEP) gene.

  • The frame-shift mutation of ABCB11 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.

Quality

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

These products are covered by the License Agreement as described in Exhibit 1 and 2, in the technical bulletin.
HepaRG is a trademark of BioPredic International company

Storage Class

12 - Non Combustible Liquids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Tristan M Sissung et al.
Molecular pharmacology, 96(2), 158-167 (2019-06-09)
Mithramycin demonstrates preclinical anticancer activity, but its therapeutic dose is limited by the development of hepatotoxicity that remains poorly characterized. A pharmacogenomics characterization of mithramycin-induced transaminitis revealed that hepatotoxicity is associated with germline variants in genes involved in bile disposition:
Xi Qiu et al.
Molecular pharmaceutics, 13(4), 1206-1216 (2016-02-26)
In the present study, we characterized in vitro biosynthesis and disposition of bile acids (BAs) as well as hepatic transporter expression followed by ABCB11 (BSEP) gene knockout in HepaRG cells (HepaRG-KO cells). BSEP KO in HepaRG cells led to time-dependent
Tristan M Sissung et al.
Molecular pharmacology, 96(2), 158-167 (2019-06-09)
Mithramycin demonstrates preclinical anticancer activity, but its therapeutic dose is limited by the development of hepatotoxicity that remains poorly characterized. A pharmacogenomics characterization of mithramycin-induced transaminitis revealed that hepatotoxicity is associated with germline variants in genes involved in bile disposition:

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 circulation.

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