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Multidrug Efflux Transporter (MDR1/P-gp) Ligand Screening Kit

Catalog #: K507
$345.00

Product Details

Cat # +Size K507-100
Size 100 Assays
Detection Method Fluorescence (Ex/Em = 488/532 nm)
Applications Screening/studying/characterizing MDR1/P-gp Inhibitors
Features & Benefits • Simple method to screen Pg-p inhibitors
• High-throughput adaptable
• Includes Inhibitor Control, Verapamil
Kit Components • Efflux Assay Buffer
• Fluorogenic P-gp Substrate
• P-gp Inhibitor (Verapamil)
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

P-glycoprotein (P-gp, Multidrug Resistance Protein 1 (MDR1), EC 3.6.3.44) 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 P-gp inhibitors is being investigated as a strategy for overcoming chemotherapy resistance. BioVision’s 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 high-throughput adaptable. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.


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Can the kit work on bacteria or yeast cells?
The kit has been standardized for mammalian cells only
What is the exact volume of sample required for this assay?
There is no specific volume we can recommend for the amount any sample to be used since it is completely sample concentration and quality based. You have to do a pilot expt with multiple sample volumes to determine the optimal volume which gives a reading within the linear range of the standard curve. Please refer to the citations for this product to see what other clients have used with similar sample types.
Do you have trial sizes of this kit?
Unfortunately, we do not have trial sizes of this kit available. However, if you are based in the US or Canada, we will give you a 10% off list price introductory discount on its purchase price. If you are based out of this area please contact your regional BioVision distributor.
What is the shelf life of this kit?
 BioVisions’s assay kits expire 6 months from the date of shipment. Some components of the kit may expire sooner as mentioned in the data sheet
Can we purchase individual components of this kit?
Yes, you can purchase any of the kit's components without the whole kit. Please refer to the component Cat #s mentioned on the datasheet for ordering.
Can we use an alternate buffer for sample preparation (cell lysis, sample dilutions etc)?
Our assay buffers are optimized for the reactions they are designed for. They not only contain some detergents for efficient lysis of your cells/tissue, but also contain some proprietary components required for the further reactions. Therefore, we highly recommend using the buffers provided in the kit for the best results.