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SBVT12

Sigma-Aldrich

SB-mouseBsep-Sf9

membrane preparation for Vesicular Transport Assays, recombinant, expressed in baculovirus infected Sf9 cells

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Synonym(s):
Bile salt export pump, Bsep, Bsep mouse vesicles, mouse Abcb11

recombinant

expressed in baculovirus infected Sf9 cells

form

liquid

concentration

5 mg/mL

color

off-white

UniProt accession no.

Q9QY30

shipped in

dry ice

storage temp.

−70°C

Gene Information

mouse ... Abcb11(27413)

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SBVT03

SB-BSEP-Hi5

form

liquid

form

liquid

form

liquid

form

liquid

concentration

5 mg/mL

concentration

5 mg/mL

concentration

5 mg/mL

concentration

5 mg/mL

UniProt accession no.

Q9QY30

UniProt accession no.

Q92887

UniProt accession no.

P33527

UniProt accession no.

O95342

shipped in

dry ice

shipped in

dry ice

shipped in

dry ice

shipped in

dry ice

storage temp.

−70°C

storage temp.

−70°C

storage temp.

−70°C

storage temp.

−70°C

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.

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

10 - Combustible liquids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Andrés E Zucchetti et al.
Molecular biology of the cell, 22(20), 3902-3915 (2011-08-26)
In estradiol 17β-d-glucuronide (E17G)-induced cholestasis, the canalicular hepatocellular transporters bile salt export pump (Abcb11) and multidrug-resistance associated protein 2 (Abcc2) undergo endocytic internalization. cAMP stimulates the trafficking of transporter-containing vesicles to the apical membrane and is able to prevent internalization
Ismael R Barosso et al.
PloS one, 7(11), e50711-e50711 (2012-12-05)
Estradiol 17ß-D-glucuronide (E17G) induces acute cholestasis in rat with endocytic internalization of the canalicular transporters bile salt export pump (Abcb11) and multidrug resistance-associated protein 2 (Abcc2). Classical protein kinase C (cPKC) and PI3K pathways play complementary roles in E17G cholestasis.
Jasminder Sahi et al.
Chemico-biological interactions, 159(2), 156-168 (2005-12-17)
CI-1034, an endothelin-A receptor antagonist was being developed for pulmonary hypertension. Drug-drug interaction studies using human hepatic microsomes were conducted to assess CYP1A2, CYP2C9, CYP2C19, CYP3A4 and CYP2D6 inhibition potential; CYP3A4 induction potential was evaluated using primary human hepatocytes. CI-1034
Emese Kis et al.
Toxicology in vitro : an international journal published in association with BIBRA, 26(8), 1294-1299 (2011-11-29)
Bile salt export pump (BSEP, ABC11) is a membrane protein that is localized in the cholesterol-rich canalicular membrane of hepatocytes. Its function is to eliminate unconjugated and conjugated bile acids/salts from hepatocyte into the bile. In humans there is no
Richard H Ho et al.
Pharmacogenetics and genomics, 20(1), 45-57 (2009-12-17)
Our aims were to identify and functionally characterize coding region nonsynonymous single nucleotide polymorphisms in the hepatic efflux transporter, bile salt export pump (BSEP; ABCB11), and to assess interindividual variability in BSEP expression. We identified 24 single nucleotide polymorphisms, including
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