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Key Documents

SBVT13

Sigma-Aldrich

SB-ratMrp2-HEK293

MRP2 rat vesicles

Sinônimo(s):

MRP2, Multidrug resistance protein 2, rat ABCC2

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About This Item

Código UNSPSC:
12352202
NACRES:
NA.84

recombinante

expressed in HEK 293 cells

forma

liquid

concentração

5 mg/mL

cor

off-white

nº de adesão UniProt

Condições de expedição

dry ice

temperatura de armazenamento

−70°C

Informações sobre genes

Descrição geral

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.

Aplicação

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 PREDIVEZTM 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.

forma física

Supplied as frozen membrane vesicles, containing 5 mg/ml membrane protein, labeled with volume, catalog number (transporter) and date of production.

Informações legais

Distributed for SOLVO Biotechnology, Inc.

Código de classe de armazenamento

10 - Combustible liquids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


Certificados de análise (COA)

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R Evers et al.
British journal of cancer, 83(3), 375-383 (2000-08-06)
The multidrug resistance proteins MRP1 and MRP2 are members of the same subfamily of ATP-binding cassette transporters. Besides organic molecules conjugated to negatively charged ligands, these proteins also transport cytotoxic drugs for which no negatively charged conjugates are known to
M G Donner et al.
Hepatology (Baltimore, Md.), 34(2), 351-359 (2001-08-02)
Cholestasis induces down-regulation of multidrug resistance protein 2 (Mrp2, symbol Abcc2), which is localized to the canalicular membrane. Given the overlapping substrate specificities of Mrp2 and multidrug resistance protein 3 (Mrp3, symbol Abcc3), we examined the hypothesis of a different
Thomas Rau et al.
Clinical pharmacology and therapeutics, 80(5), 468-476 (2006-11-23)
The adenosine triphosphate-binding cassette (ABC) class transporter ABCC2 (MRP2 [multidrug resistance related protein 2] or cMOAT [canalicular multispecific organic anion transporter]) is involved in the cellular outward transport and elimination of methotrexate. We hypothesized that common genetic variations may contribute
Isabelle Benz-de Bretagne et al.
Journal of biomedicine & biotechnology, 2011, 498757-498757 (2011-05-05)
MRP2 encoded by ABCC2 gene is involved in the secretion of numerous drugs and endogenous substrates. Patients with Dubin-Johnson syndrome due to mutation in ABCC2 gene have elevated urinary coproporphyrin ratio (UCP I/(I + III)). Here we investigated whether this
Potentiation of MRP2/Mrp2-mediated estradiol-17beta-glucuronide transport by drugs--a concise review.
Krisztina Herédi-Szabó et al.
Chemistry & biodiversity, 6(11), 1970-1974 (2009-11-26)

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