SBAT02
MRP1 human
membrane preparation for ATPase Assay, recombinant, expressed in baculovirus infected Sf9 cells
Synonyme(s) :
ABCC1, Multidrug resistance-associated protein 1
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About This Item
Code UNSPSC :
12352202
Nomenclature NACRES :
NA.84
Produit recombinant
expressed in baculovirus infected Sf9 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 ... ABCC1(4363)
Description générale
Membrane Preparations for ATPase Assays are suitable for drug-efflux transporter interaction studies based on ATPase activity determination, and could be used for differentiation between transporter substrates and inhibitors.
Application
The ATPase assay is an in vitro membrane assay designed to indicate the nature of the interaction between the compound and the transporter. By measuring ATPase activity, both activation and inhibition of transporters can be investigated using membranes from baculovirus-infected insect cells or mammalian cell membranes containing high levels of human or rodent wild-type transporters. ABC transporters mediate the transport of substrates against a concentration gradient using energy derived from ATP hydrolysis, which is proportional to the transporter activity and could easily be detected with a colorimetric method.
To assess activation, ABC transporter-rich membranes are incubated with various (typically in 8) concentrations of the test article and the effect on basal ATPase activity is measured. Compounds that stimulate ATPase are generally considered substrates for the transporter. To assess inhibition, a test article′ ability to modify the activity of a given ABC transporter stimulated with its prototypical substrates is examined. The activation and inhibition tests are complementary assays.
Stimulation detected in the activation assay indicate that the compound is a transported substrate of the transporter, while interactions detected in the inhibition test indicate interaction of the test compounds with the transporter, but do not give information on the nature (substrate or inhibitor) of the interaction. In some cases inhibitors or slowly transported compounds may inhibit the baseline transporter ATPase activity as well.
Slowly transported substrates often do not stimulate the ATPase activity in a detectable extent; however the existing interaction can be identified in the inhibition assay.
To assess activation, ABC transporter-rich membranes are incubated with various (typically in 8) concentrations of the test article and the effect on basal ATPase activity is measured. Compounds that stimulate ATPase are generally considered substrates for the transporter. To assess inhibition, a test article′ ability to modify the activity of a given ABC transporter stimulated with its prototypical substrates is examined. The activation and inhibition tests are complementary assays.
Stimulation detected in the activation assay indicate that the compound is a transported substrate of the transporter, while interactions detected in the inhibition test indicate interaction of the test compounds with the transporter, but do not give information on the nature (substrate or inhibitor) of the interaction. In some cases inhibitors or slowly transported compounds may inhibit the baseline transporter ATPase activity as well.
Slowly transported substrates often do not stimulate the ATPase activity in a detectable extent; however the existing interaction can be identified in the inhibition assay.
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)
Code de la classe de stockage
12 - Non Combustible Liquids
Classe de danger pour l'eau (WGK)
WGK 1
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".
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S-M He et al.
Current medicinal chemistry, 18(3), 439-481 (2010-12-15)
Multidrug ABC transporters such as P-glycoprotein (P-gp/MDR1/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1) play an important role in the extrusion of drugs from the cell and their overexpression can be a cause of failure of anticancer and antimicrobial chemotherapy. Recently
Roger G Deeley et al.
Physiological reviews, 86(3), 849-899 (2006-07-04)
Multidrug Resistance Proteins (MRPs), together with the cystic fibrosis conductance regulator (CFTR/ABCC7) and the sulfonylurea receptors (SUR1/ABCC8 and SUR2/ABCC9) comprise the 13 members of the human "C" branch of the ATP binding cassette (ABC) superfamily. All C branch proteins share
J Wijnholds et al.
Nature medicine, 3(11), 1275-1279 (1997-11-14)
The multidrug resistance-associated protein (MRP) mediates the cellular excretion of many drugs, glutathione S-conjugates (GS-X) of lipophilic xenobiotics and endogenous cysteinyl leukotrienes. Increased MRP levels in tumor cells can cause multidrug resistance (MDR) by decreasing the intracellular drug concentration. The
Cornelius F H Mueller et al.
Circulation research, 97(7), 637-644 (2005-08-27)
Glutathione (GSH) is the major source of intracellular sulfhydryl groups. Oxidized GSH (GSSG) can be recycled to GSH by the GSH reductase or exported from the cell. The mechanism by which GSSG is exported and the consequence of its export
Eva Bakos et al.
Pflugers Archiv : European journal of physiology, 453(5), 621-641 (2006-12-26)
MRP1 (ABCC1) is a peculiar member of the ABC transporter superfamily for several aspects. This protein has an unusually broad substrate specificity and is capable of transporting not only a wide variety of neutral hydrophobic compounds, like the MDR1/P-glycoprotein, but
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