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Sigma-Aldrich

HepaRG Cells BCRP (-/-)

human female liver (hepatocarcinoma and hepatitis C tumor)

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About This Item

UNSPSC Code:
12352207

product name

HepaRG Cells BCRP (-/-), one vial

biological source

human female liver (hepatocarcinoma and hepatitis C tumor)

Quality Level

form

liquid

OMIM accession no.

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.

Application

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.

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

Exhibit 1: ADME/Tox cell lines license
Exhibit 2: HepaRG limited use license
HepaRG is a trademark of BioPredic International company

Disclaimer

RESEARCH USE ONLY. This product is regulated in France when intended to be used for scientific purposes, including for import and export activities (Article L 1211-1 paragraph 2 of the Public Health Code). The purchaser (i.e. enduser) is required to obtain an import authorization from the France Ministry of Research referred in the Article L1245-5-1 II. of Public Health Code. By ordering this product, you are confirming that you have obtained the proper import authorization.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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Jiska Jebbink et al.
Biochimica et biophysica acta, 1852(1), 131-136 (2014-12-03)
To investigate total bile acid (TBA) levels in maternal (MB) and umbilical cord blood (UCB) in normotensive, preeclamptic (PE), and PE pregnancies complicated by hemolysis elevated liver enzymes and low platelets (HELLP) syndrome in the context of ABCG2 placental gene
Wei-Chien Huang et al.
PloS one, 8(12), e83627-e83627 (2014-01-07)
The multikinase inhibitor, sorafenib (Nexavar®, BAY43-9006), which inhibits both the Raf/MEK/ERK pathway and several receptor tyrosine kinases (RTKs), has shown significantly therapeutic benefits in advanced hepatocellular carcinoma (HCC). However, not all HCC patients respond to sorafenib well and new therapeutic
Zoe Riches et al.
Chemico-biological interactions, 242, 203-210 (2015-10-16)
The aim of this study was to characterize the ontogeny and variability of the BCRP (ABCG2) transporter in healthy human liver. Levels of BCRP mRNA and protein were determined with q-RT-PCR and western blot in a cohort of 87 human
A Pál et al.
The Journal of pharmacology and experimental therapeutics, 321(3), 1085-1094 (2007-03-10)
ABCG2, a transporter of the ATP-binding cassette family, is known to play a prominent role in the absorption, distribution, metabolism, and excretion of xenobiotics. Drug-transporter interactions are commonly screened by high-throughput systems using transfected insect and/or human cell lines. The
Satoshi Benoki et al.
Archives of biochemistry and biophysics, 517(2), 123-130 (2011-11-19)
A previous report demonstrated that treatment of human hepatocytes with phenobarbital, an activator of nuclear receptor constitutive androstane receptor (CAR), increases mRNA levels of an efflux transporter ABCG2, which is involved in the excretion of xenobiotics in liver and intestine.

Articles

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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