Human Transporter MRP2 Fluorescence-based Antagonist Assay Service
Human Transporter MRP2 Fluorescence-based Antagonist Assay is a laboratory test used to evaluate the inhibitory effects of a substance on the multidrug resistance protein 2 (MRP2) transporter in human cells. MRP2 is a membrane protein that plays a key role in the transport of various drugs and toxins out of cells, thus contributing to drug resistance in cancer cells and other cell types.
MRP2
MRP2 protein, also known as Multidrug Resistance-Associated Protein 2, is a transmembrane protein that is involved in the transport of a wide range of endogenous and xenobiotic substrates across the cell membrane. It is a member of the ATP-binding cassette (ABC) transporter family and is primarily expressed in the liver, kidneys, and intestines. MRP2 plays a crucial role in the elimination of toxic compounds and metabolites from the body by transporting them out of cells and into bile or urine for excretion. It is also involved in the transport of a variety of drugs, leading to multidrug resistance in cancer cells and affecting the pharmacokinetics of various medications.
Our Service
In this assay, human cells expressing MRP2 are exposed to a known substrate of the transporter, such as 5(6)-carboxy-2',7'-dichlorofluorescein (CDCF). The test substance being evaluated for its antagonist effects on MRP2 is added to the cells, and the intracellular accumulation of the substrate is measured using fluorescence detection methods. By quantifying the levels of the substrate inside the cells in the presence of the test substance, you can determine the ability of the substance to inhibit the transport function of MRP2.
Detection Method
Fluorimetry
Functional Mode
Antagonist
Measured Response
Fluorescence
1
Prepare a stock solution of the MRP2 human transporter inhibitor to be tested.
2
Plate a monolayer of MRP2-overexpressing cells in 96-well plates.
3
Allow the cells to adhere and grow for 24 hours.
4
Prepare a range of concentrations of the MRP2 inhibitor in culture media.
5
Add the MRP2 inhibitor solutions to the cells and incubate.
6
Prepare a stock solution of the CDCF substrate and dilute it in culture media.
7
Add the CDCF substrate to the cells and incubate for a specific period.
8
Measure the fluorescence intensity of the CDCF substrate.
9
Calculate the efflux activity of MRP2 by measuring the decrease in CDCF substrate fluorescence intensity.
10
Generate a dose-response curve by plotting the efflux activity against the concentration of the MRP2 inhibitor.
11
Determine the IC50 value of the MRP2 inhibitor.
12
Analyze the data to assess the potency and efficacy of the MRP2 inhibitor.
Applications
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Screen potential drug compounds for their ability to inhibit the MRP2 transporter.
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Assess the potential toxicity of new drug compounds by measuring their effects on MRP2 transporter activity.
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Study the impact of drug compounds on the transport of endogenous substrates by MRP2 in the liver and other tissues.
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Study genetic variations in the MRP2 transporter gene that may affect drug response and toxicity in individuals.
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Investigate the role of MRP2 in multidrug resistance in cancer cells.
Advantages
Provides a highly specific method for studying the interaction of compounds with the MRP2 transporter protein.
Have predictive value for assessing the potential toxicity of drugs in humans.
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High throughput screening
Allows you to quickly screen many compounds for their effects on MRP2 activity.
Study various compounds, including pharmaceuticals, environmental toxins, and natural products.
Why Choose Creative Biolabs
Other Services at Creative Biolabs
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Contact Us
If you are interested in learning more about our Human Transporter MRP2 Fluorescence-based Antagonist Assay Service, please do not hesitate to contact us. Our team of experts will be happy to provide you with all the information you need and answer any questions you may have. Whether you are looking to inquire about pricing, turnaround time, or any other aspect of our assay service, we are here to assist you.
For Research Use Only | Not For Clinical Use
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