Address: 45-1 Ramsey Road, Shirley, NY 11967, USA    USA: 1-631-559-9269  1-631-448-7888   Fax: 1-631-938-8127  Europe: 44-207-097-1828   Email:
Home > Products > Assay Kits > Activity Kits > Multidrug Efflux Transporter Ligand Screening Kit

Multidrug Efflux Transporter Ligand Screening Kit

"MDR1" Related Products.
Product Overview:
The MDR1/P-gp Ligand Screening Kit is designed for rapidly screening test compounds for modulation of efflux transporter activity in MDR1-expressing cell lines. The assay uses a lipophilic non-fluorescent P-gp substrate that readily diffuses through the plasma membrane, where it is hydrolyzed to an active fluorophore by cytosolic esterases. The resulting hydrophilic fluorophore is neither membrane permeable nor a substrate for P-gp, hence it remains trapped inside the cell. In MDR1-expressing cell lines, the lipophilic pro-fluorophore is continuously extruded from the cytosol by P-gp, leading to a low intracellular fluorescence. Inhibition of P-gp-mediated efflux by a test compound leads to increased intracellular fluorescence. Specific transporter activity is quantified by comparison with fluorescence accumulated in the presence and absence of a saturating concentration of the included selective P-gp inhibitor. The assay is highly sensitive, has a simple no-wash protocol and is highthroughput adaptable. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.
100 assays
P-glycoprotein (P-gp, Multidrug Resistance Protein 1 (MDR1), EC is a member of the ATP-binding cassette (ABC) ATPase superfamily of transmembrane transporter proteins. P-gp has an extremely broad substrate specificity and is capable of transporting a vast array of neutral and anionic lipophilic molecules. P-gp strongly affects the oral absorption, tissue distribution and excretion of many drugs and prevents certain lipophilic drugs from penetrating the blood brain barrier. Overexpression of P-gp confers tumor cells with resistance to chemically and pharmacologically distinct chemotherapeutic drugs (such as doxorubicin, vincristine and paclitaxel) by actively pumping them out of cells. Induction of P-gp expression is a frequent cause of treatment failure and tumor-targeted delivery of Pgp inhibitors is being investigated as a strategy for overcoming chemotherapy resistance.
Screening and characterization of drugs and new chemical entities for inhibition of native/recombinant MDR1/P-gp efflux transporter.Identification/characterization of cells and cell lines with a high level of MDR1-mediated efflux (i.e. chemotherapy-resistant).
Store kit at -20°C and protect from light. Briefly centrifuge all small vials prior to opening. Open all of the reagents under sterile conditions (e.g. a cell culture hood) only. Read entire protocol before performing the assay procedure.Efflux Assay Buffer: Allow to thaw to room temperature under sterile conditions. Store at 4°C.Fluorogenic P-gp Substrate: Reconstitute with 55 µl anhydrous DMSO and vortex thoroughly to obtain a 400X stock solution. Aliquot the stock solution as desired and store aliquots at -20°C, protected from light. Avoid repeated freeze/thaw cycles.P-gp Inhibitor (Verapamil): Reconstitute with 110 µl anhydrous DMSO and vortex until fully dissolved to obtain a 100X stock solution. Store at -20°C, stable for at least 4 freeze/thaw cycles.
Kit Components:
Efflux Assay Buffer: 50 mlFluorogenic P-gp Substrate: 1 vialP-gp Inhibitor (Verapamil): 1 via
Detection method:
Fluorescence (Ex/Em = 488/532 nm)
Compatible Sample Types:
Cells expressing high levels of MDR1/P-gp (e.g. cancer cell line with cytotoxic drug-resistant phenotype)
Features & Benefits:
• Simple method to screen P-gp inhibitors• High-throughput adaptable• Includes Inhibitor Control, Verapamil

Online Inquiry    
Note: There will be extra charge for optional service!
Optional requirements on this protein +Expand
C-fusion   N-fusion  Non-tagged
His   GST  Fc  Others
<1.0 eu/μg   <0.1 eu/μg  <0.01 eu/μg  Not required
Monomer Isolation   Dimer Isolation   Not required
>80% by SDS-PAGE   >90% by SDS-PAGE  >95% by SDS-PAGE  Others
Please input "biomart" as verification code.
Please review Creative Biomart's privacy policy for more information.
Price does not include shipping and packaging costs.Request quote for final price.

If you have any other questions, please call

online inquiry

Welcome! For price inquiries, please feel free to contact us through the form below. We will get back to you as soon as possible.

45-1 Ramsey Road, Shirley, NY 11967, USA
USA: 1-631-559-9269  1-631-448-7888
Europe: 44-207-097-1828
FAX: 1-631-938-8127

facebook twitter linkedin google plus google plus

Join 10 other subscribers

Easy access to products and services you need from our library via powerful searching tools
Copyright © 2007 - 2017 Creative Biomart. All Rights Reserved.