SBVT09

Sigma-Aldrich

SB-BCRP-M

recombinant, expressed in human cells (expressed in proprietary human “M” cells)

Sinónimos:
ABCG2, Breast Cancer Resistance Protein, BCRP, BCRP human membrane vesicles
En este momento no podemos mostrarle ni los precios ni la disponibilidad

recombinant

expressed in human cells (expressed in proprietary human “M” cells)

form

liquid

concentration

5.0 mg/mL

color

off-white

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

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.

RIDADR

NONH for all modes of transport

WGK Germany

WGK 2

Flash Point F

Not applicable

Flash Point C

Not applicable

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...
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...
Márton Jani et al.
Journal of pharmaceutical sciences, 100(1), 94-97 (2010-06-25)
Ivermectin is an antiparasitic drug frequently administered to humans. It has a limited brain exposure that is attributed to the efflux activity of ABCB1/Abcb1. ABCG2/Abcg2 is also a major transporter present in most pharmacologically important barriers. However, interaction of ivermectin...
E Kis et al.
Annals of the rheumatic diseases, 68(7), 1201-1207 (2008-04-10)
Earlier publications have suggested a possible role for the efflux transporter breast cancer resistance protein (BCRP) in acquired resistance to disease-modifying antirheumatic drugs (DMARDs) such as leflunomide and its metabolite A771726 (teriflunomide). However, there is no direct evidence that BCRP...
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....

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