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SBVT01

Sigma-Aldrich

SB-MDR1-K

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

Synonym(s):

ABCB1, MDR1, MDR1 human membrane vesicles, Multidrug resistance-associated protein 1, Pgp

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About This Item

UNSPSC Code:
12352200

recombinant

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

form

liquid

concentration

5 mg/mL

color

off-white

UniProt accession no.

shipped in

dry ice

storage temp.

−70°C

Gene Information

human ... ABCB1(5243)

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 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.

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 MDR1/P-gp part number SBPVR1-9RXN and corresponding control membrane SB K CTRL part number SBCT01-1EA

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.

Storage Class Code

12 - Non Combustible Liquids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Ya-tong Zhang et al.
British journal of clinical pharmacology, 66(2), 240-246 (2008-08-23)
Ciclosporin (CsA), which is widely used in autoimmune disease and transplantation, has a narrow therapeutic index. It also shows considerable interindividual variability in its pharmacokinetics, which may be attributable to polymorphisms of the multidrug efflux pump P-glycoprotein, encoded by MDR-1.
MDR1, the blood-brain barrier transporter, is associated with Parkinson's disease in ethnic Chinese.
C G L Lee et al.
Journal of medical genetics, 41(5), e60-e60 (2004-05-04)
R B Wang et al.
Journal of clinical pharmacy and therapeutics, 28(3), 203-228 (2003-06-11)
A large number of structurally and functionally diverse compounds act as substrates or modulators of p-glycoprotein (p-gp). Some of them possess multiple drug resistance (MDR)-reversing activity, but only a small number of them have entered clinical study. In order to
Zsuzsanna Rajnai et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(11), 2000-2006 (2010-08-12)
Seliciclib, a cyclin-dependent kinase inhibitor, is a promising candidate to treat a variety of cancers. Pharmacokinetic studies have shown high oral bioavailability but limited brain exposure to the drug. This study shows that seliciclib is a high-affinity substrate of ATP-binding
Drug-drug interactions of new active substances: mibefradil example.
M Siepmann et al.
European journal of clinical pharmacology, 56(3), 273-273 (2000-08-22)

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