Caco-2-based BCRP Substrate Assessment Service
Our Caco-2-based BCRP substrate assessment service offers a comprehensive evaluation of compounds to determine their affinity for BCRP, a member of the ABC transporter family that plays a crucial role in drug efflux and resistance.
BCRP
Breast cancer resistance protein (BCRP) is a protein that belongs to the ATP-binding cassette (ABC) transporter family. This protein is encoded by the ABCG2 gene and is primarily found in the cell membrane of various tissues, including the liver, intestine,
kidney, and placenta. BCRP plays a crucial role in the efflux of a wide range of substrates, including drugs, toxins, and metabolites, out of cells. This efflux activity helps to protect cells from the harmful effects of these substances and also
plays a role in drug resistance in cancer cells.
Caco-2-based BCRP Substrate Assessment Service
Our service involves testing compounds using Caco-2 cells, an established human epithelial colorectal adenocarcinoma cell line commonly used in drug permeability studies. By assessing the transcellular transport of compounds across Caco-2 monolayers over
a specified period of time, we are able to determine their substrate potential for BCRP. Here's the specific information about this service:
Process of Our Service
1
Cell Culture Maintenance
Caco-2 cells are cultured and maintained in an appropriate cell culture medium under controlled conditions to ensure their viability and growth.
2
Differentiation
Caco-2 cells are allowed to differentiate on permeable supports to form tight junctions and develop characteristics resembling the intestinal epithelium.
3
Transport Studies
The potential BCRP substrate is added to the apical or basolateral compartment of the system, and its transport across the Caco-2 cell monolayer is assessed over a specific period of time.
4
Inhibition Studies
To evaluate the involvement of BCRP in the transport of the substrate, specific BCRP inhibitors can be added to the system to determine their effect on the transport process.
5
Data Analysis
The amount of substrate transported across the Caco-2 cell monolayer is quantified, and the Papp is calculated to determine the transport characteristics of the substrate.
6
Interpretation
The data obtained from the transport studies are analyzed to assess whether the potential substrate is a BCRP substrate based on its transport properties and the impact of BCRP inhibitors.
7
Reporting
A detailed report summarizing the experimental procedures, results, and interpretation of the findings is provided to the client.
The results of our assessment can provide valuable insights into the likelihood of a compound being actively effluxed by BCRP, which can impact its bioavailability, pharmacokinetics, and efficacy. This information is essential for drug development and
can help guide decision-making in the selection of lead compounds for further development.
Assay Information
Assay Sub Type
Cell Based
Detection Method
HPLC-MS/MS
Measured Response
Peak Area Response
Features of Our Service
-
High-quality Caco-2 cell-based model
Our service utilizes Caco-2 cells for assessing drug transport across the intestinal epithelium.
-
Evaluation of BCRP substrate potential
Our service assesses the potential of a drug candidate to be a substrate for BCRP.
-
Accurate measurement of transport parameters
This assay allows for the determination of key transport parameters, such as apparent permeability (Papp) values.
Contact Us
With our expertise and state-of-the-art equipment, we offer reliable and accurate assessment services to support your drug development efforts. Contact us now to learn more about our Caco-2-based BCRP substrate assessment
service and how we can assist you in evaluating the transport properties of your compounds.
For Research Use Only | Not For Clinical Use
Download our brochure