Understanding interactions of potential drug candidates with MRP3 is vital for elucidating their pharmacokinetic properties and ensuring efficacy and safety. Creative Biolabs offers a state-of-the-art MRP3 Fluorescence-Based Antagonist Assay Service, utilizing cutting-edge technologies for efficient and reliable transporter interaction studies.

Background of MRP3

Multidrug resistance-associated protein 3 (MRP3), part of the ATP binding cassette (ABC) transporter family, plays a significant role in the efflux of bilirubin glucuronides, bile acids, and xenobiotics. Functioning in a unidirectional, ATP-dependent manner, MRP3 is critical in hepatocyte relief, particularly under cholestatic conditions. First identified in the liver at the sinusoidal membrane, MRP3 is also expressed in the gastrointestinal tract, adrenal gland, kidney, pancreas, placenta, and other tissues. The transporter's study has vital implications for understanding drug absorption, disposition, drug-drug interactions (DDIs), and potential therapeutic strategies.

Fig.1 Schematic of MRP3 structure.^1,2

Human Transporter MRP3 Fluorescence-based Antagonist Assay Service at Creative Biolabs

At Creative Biolabs, we offer a high-precision MRP3 Fluorescence-based Antagonist Assay, designed to screen and profile compounds that interact with the MRP3 transporter. By leveraging fluorescence detection methods, our assay provides a cost-effective, reliable platform for assessing the antagonist activity against MRP3. This service aids in identifying potential inhibitors, understanding their pharmacokinetics, and ensuring the safety and efficacy of novel drug candidates.

Service Details

Our assay is performed on HEK293 cells expressing full-length human MRP3 protein utilizing advanced spectrophotometric techniques, ensuring physiological relevance and high accuracy.

• Substrate: 20 µM of CDCF (5-carboxy-2,7-dichlorofluorescein).
• Incubation: 35 minutes at 37 °C.
• Criteria for Significance: 25% inhibition.
• Testing Information: Suggested dose-response study with 8-dose concentrations in duplicate.

Applications of Human Transporter MRP3 Fluorescence-based Antagonist Assay

The MRP3 fluorescence-based antagonist assay has a wide array of applications in drug discovery and development, including:

• Drug Screening and Profiling: Identify and characterize novel inhibitors of MRP3, assessing their potential impact on drug efficacy and safety.
• Pharmacokinetic Studies: Evaluate the role of MRP3 in the absorption, distribution, metabolism, and excretion (ADME) processes of new drug candidates.
• Drug-Drug Interaction Studies: Investigate potential DDIs involving MRP3, crucial for understanding synergistic or antagonistic effects when co-administering multiple drugs.
• Therapeutic Strategy Development: Guide the development of therapies for conditions associated with MRP3 dysfunction, such as cholestasis or multidrug resistance in cancers.

Highlights of Our Service

• High Sensitivity and Specificity: Our assay employs highly sensitive fluorescence detection, enabling the detection of MRP3 interactions even at low inhibitor concentrations.
• Regulatory Compliance: Our assay methodology aligns with various guidelines, ensuring robust data for regulatory submissions.
• Efficiency and Cost-effectiveness: Utilizing fluorescence probes, our service is faster and more cost-effective compared to traditional radioactive probes, without compromising sensitivity.
• Comprehensive Analysis: Our service includes detailed data analysis and interpretation, providing insights into the potential implications of observed interactions.

Frequently Asked Questions

Q1: Why is MRP3 important in drug development?

A1: MRP3 is pivotal in the efflux of drugs and their metabolites, significantly affecting their pharmacokinetics and safety profiles. Understanding MRP3 interactions helps predict potential DDIs and guides dosage adjustments for optimal therapeutic efficacy.

Q2: How does the fluorescence-based method compare with traditional techniques?

A2: Fluorescence-based methods are generally more sensitive and cost-effective compared to radioactive probes. They provide a safer, faster, and equally reliable alternative for transporter interaction studies.

At Creative Biolabs, our Human Transporter MRP3 Fluorescence-based Antagonist Assay Service sets the benchmark for high-quality, reliable, and cost-effective transporter interaction studies. By integrating advanced fluorescence techniques, regulatory compliance, and comprehensive analysis, we support your drug development journey from discovery to market. Learn more about our services and how we can assist in optimizing your drug candidates for safety and efficacy.

References

1. Kuan, Chien-Tsun, et al. "MRP3: a molecular target for human glioblastoma multiforme immunotherapy." BMC cancer 10 (2010): 1-15.
2. Distributed under Open Access License CC BY 4.0, without modification.

For Research Use Only | Not For Clinical Use