MDCKII-based P-gp Substrate Assessment Service
Our MDCKII-based P-gp substrate assessment service utilizes the Madin-Darby Canine Kidney Type II (MDCKII) cell line to assess the permeability of compounds through P-glycoprotein (P-gp), a drug transporter protein that plays a key role in determining
the absorption, distribution, and elimination of drugs in the body.
P-glycoprotein
P-gp, or P-glycoprotein, is a protein found in the membrane of cells that functions as an efflux pump, actively transporting various substances out of cells. Substances that are substrates of P-gp are actively pumped out of cells, leading to reduced intracellular
concentration and potentially affecting the efficacy of drugs that rely on cellular uptake. It is important to consider P-gp substrate status when designing drug therapies, as the presence of P-gp can affect drug absorption, distribution, and
elimination. To assess whether a drug is a substrate of P-gp, a commonly used cell model is the MDR1-MDCKII cell line, which overexpresses the human P-gp protein.
MDCKII-based P-gp Substrate Assessment Service
We use stable MDCKII cell lines overexpressing P-gp to assess the permeability and efflux of your compound compared to known P-gp substrates. This will provide you with valuable information about the likelihood of your compound becoming a substrate for
P-gp and the potential drug-drug interactions or poor bioavailability. Here's the specific information about this service:
Assay Information
Measured Response
Peak Area Response
Process of Our Service
1
Culturing of MDR1-MDCKII cells
The MDR1-MDCKII cells are grown in culture dishes under appropriate conditions to ensure their growth and maintenance.
2
Treatment with the test drug
The test drug is added to the MDR1-MDCKII cells at a specified concentration and incubated for a certain period of time.
3
Measurement of drug accumulation
Following treatment with the test drug, the intracellular accumulation of the drug in the MDR1-MDCKII cells is measured using various analytical techniques such as LC-MS.
4
Comparison with control cells
The level of drug accumulation in the MDR1-MDCKII cells is compared with control cells that do not express P-gp to determine the efflux of the drug by P-gp.
5
Data analysis
The results from the drug accumulation studies are analyzed to determine whether the test drug is a substrate of P-gp.
If the test drug shows substantially lower intracellular accumulation in the MDR1-MDCKII cells compared to the control cells, it is likely to be a substrate of P-gp. This assay is valuable for understanding the potential for drug-drug interactions and
designing strategies to overcome MDR in cancer treatment.
Advantages of Our Service
Assessing whether a drug is a P-gp substrate can help predict potential drug interactions with other medications that are also P-gp substrates.
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Predicting drug absorption and distribution
Understanding a drug's P-gp substrate status can help predict its pharmacokinetics and overall effectiveness.
Assessing whether a drug is a P-gp substrate can help identify potential resistance mechanisms and develop strategies to overcome them.
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Research and drug development
Identifying P-gp substrates can aid in the early stages of drug development by informing decisions about compound selection and optimization.
Frequently Asked Question
A1: What is the timeline of the MDCKII-based P-gp substrate evaluation service?
Q1: The timeline of the MDCKII-based P-gp substrate evaluation service can vary depending on the specific protocol and requirements of the evaluation. Overall, the timeline for the MDCKII-based P-gp substrate evaluation service may range from 3 to 5 weeks,
depending on the complexity of the evaluation and the specific requirements of the client.
Contact Us
Contact us today to learn more about our MDCKII-based P-gp substrate assessment service and how we can assist in advancing your research and development projects.
For Research Use Only | Not For Clinical Use
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