SBVT01
SB-MDR1-K
recombinant, expressed in human cells (proprietary human “K” cells)
Synonyme(s) :
ABCB1, MDR1, MDR1 human membrane vesicles, Multidrug resistance-associated protein 1, Pgp
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About This Item
Code UNSPSC :
12352200
Produits recommandés
Produit recombinant
expressed in human cells (proprietary human “K” cells)
Forme
liquid
Concentration
5 mg/mL
Couleur
off-white
Numéro d'accès UniProt
Conditions d'expédition
dry ice
Température de stockage
−70°C
Informations sur le gène
human ... ABCB1(5243)
Description générale
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
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
Forme physique
Supplied as frozen membrane vesicles, containing 5 mg/ml membrane protein, labeled with volume, catalog number (transporter) and date of production.
Informations légales
Distributed for SOLVO Biotechnology, Inc.
Produit(s) apparenté(s)
Réf. du produit
Description
Tarif
Code de la classe de stockage
12 - Non Combustible Liquids
Classe de danger pour l'eau (WGK)
WGK 2
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.
Siegfried Drescher et al.
British journal of clinical pharmacology, 53(5), 526-534 (2002-05-08)
The C3435T polymorphism in the human MDR1 gene is associated with lower intestinal P-glycoprotein expression, reduced protein function in peripheral blood cells and higher plasma concentrations of the P-glycoprotein substrate digoxin. Using fexofenadine, a known P-glycoprotein substrate, the hypothesis was
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)
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)
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
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
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
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