SBVT09
SB-BCRP-M
recombinant, expressed in human cells (expressed in proprietary human “M” cells)
Synonym(s):
ABCG2, BCRP, BCRP human membrane vesicles, Breast Cancer Resistance Protein
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About This Item
UNSPSC Code:
12352200
Recommended Products
recombinant
expressed in human cells (expressed in proprietary human “M” cells)
form
liquid
concentration
5.0 mg/mL
color
off-white
UniProt accession no.
shipped in
dry ice
storage temp.
−70°C
Gene Information
human ... ABCG2(9429)
General description
Membrane Preparations for Vesicular Transport Assays (VT) are suitable for general drug-efflux transporter interaction studies. Both substrate and inhibitor interactions can be assessed using vesicles. The success of substrate interaction studies strongly depends on the passive permeability of the compound. High permeability substrates might not be detected. Control Membranes with no-, or significantly lower transporter activity are also available.
Application
In the vesicular transport assay so-called "inside-out" membrane vesicles containing ABC transporters are applied. Incubating substrates of the respective efflux transporter in the presence of the inverted membrane vesicles and ATP will allow measuring accumulation of the substrates into the vesicles. In many cases radiolabeled reporter substrates are used but recently SOLVO developed the new PREDIVEZ Vesicular Transport Kits that use fluorescent reporter substrates.
The standard vesicular transport assay is an inhibitory assay performed with cold test articles. This assay provides information on any interaction between the ABC transporter and the test article. The transport of the reporter substrate is measured in the presence of the test article (typically in 7 concentrations) and IC50 is defined as the concentration inhibiting the transport of the reporter substrate by 50%.
Should radiolabeled form of the investigated compound or adequate analytical methods (LC/MS, HPLC) be available, the vesicular transport assay may be performed in a direct format without the reporter substrate and may identify substrate nature of the test article. The vesicular transport substrate assay is a low throughput assay. It is suitable for low permeability test compounds as high permeability compounds may escape from the vesicles through the lipid bilayer.
PREDIVEZ vesicular transport kit is sold separately. This transporter membrane vesicle assay requires the PREDIVEZ vesicular transport kit and corresponding control membrane below:
SB PREDIVEZ Reagent Kit for BCRP part number SBPVR4-9RXN and corresponding control membrane SB-M-CTRL part number SBCT02-1EA
The standard vesicular transport assay is an inhibitory assay performed with cold test articles. This assay provides information on any interaction between the ABC transporter and the test article. The transport of the reporter substrate is measured in the presence of the test article (typically in 7 concentrations) and IC50 is defined as the concentration inhibiting the transport of the reporter substrate by 50%.
Should radiolabeled form of the investigated compound or adequate analytical methods (LC/MS, HPLC) be available, the vesicular transport assay may be performed in a direct format without the reporter substrate and may identify substrate nature of the test article. The vesicular transport substrate assay is a low throughput assay. It is suitable for low permeability test compounds as high permeability compounds may escape from the vesicles through the lipid bilayer.
PREDIVEZ vesicular transport kit is sold separately. This transporter membrane vesicle assay requires the PREDIVEZ vesicular transport kit and corresponding control membrane below:
SB PREDIVEZ Reagent Kit for BCRP part number SBPVR4-9RXN and corresponding control membrane SB-M-CTRL part number SBCT02-1EA
Physical form
Supplied as frozen membrane vesicles, containing 5 mg/ml membrane protein, labeled with volume, catalog number (transporter) and date of production.
Legal Information
Distributed for SOLVO Biotechnology, Inc.
related product
Product No.
Description
Pricing
Storage Class
12 - Non Combustible Liquids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Albert Mennone et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(10), 1673-1678 (2010-07-06)
Breast cancer resistance protein (Bcrp) is a member of the ATP-binding cassette membrane transporter family, which is expressed apically in liver, kidney, and intestine epithelium. Recent reports suggest that in addition to xenobiotics, porphyrins, and food toxins, Bcrp can also
M Maliepaard et al.
Cancer research, 61(8), 3458-3464 (2001-04-20)
High expression of the Breast Cancer Resistance Protein (BCRP) gene has been shown to be involved in resistance to chemotherapeutic drugs. Knowledge of the localization of BCRP protein in normal tissues may help unravel the normal function of this protein.
Márton Jani et al.
Biological & pharmaceutical bulletin, 32(3), 497-499 (2009-03-03)
The pharmacokinetics of sulfasalazine, an anti-inflammatory drug is influenced by ATP-binding cassette G2 (ABCG2) (breast cancer resistance protein (BCRP), mitoxantrone resistance protein (MXR)) both in vitro and clinically. Due to its low passive permeability, the intracellular concentration of sulfasalazine is
Hiroshi Kodaira et al.
The Journal of pharmacology and experimental therapeutics, 333(3), 788-796 (2010-03-23)
A synergistic effect of P-glycoprotein (P-gp)/Abcb1a and breast cancer resistance protein (Bcrp)/Abcg2 was reported to limit the brain penetration of their common substrates. This study investigated this based on pharmacokinetics using Mdr1a/1b(-/-), Bcrp(-/-), and Mdr1a/1b(-/-)/Bcrp(-/-) mice. Comparison of the brain-
Kumie Kage et al.
International journal of cancer, 97(5), 626-630 (2002-01-25)
Breast cancer resistance protein (BCRP) is a half-molecule ABC transporter highly expressed in mitoxantrone-resistant cells. In our study we established PA317 transfectants expressing Myc-tagged BCRP (MycBCRP) or HA-tagged BCRP (HABCRP). The exogenous BCRP protein migrated as a 70-kDa protein in
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