Human BCRP Vesicle Kit
HEK293-derived inside-out membrane vesicles for BCRP inhibition screening and drug-drug interaction (DDI) risk assessment, in line with FDA and EMA testing recommendations.
Core Regulatory Transporter
Included in FDA and EMA DDI transporter panels alongside P-gp as a standard efflux assessment.
Inside-Out Vesicles
HEK293-derived membrane vesicles with confirmed BCRP expression and inside-out orientation for reliable, reproducible transport data.
100 Reactions per Kit
Each kit is sized for 100 reactions based on a 96-well plate format, suitable for IC50 determination and single-concentration screening.
Dry Ice Shipment
Shipped frozen at −80 °C on dry ice to preserve vesicle integrity and transport activity upon arrival.
Why BCRP testing matters in DMPK programs
BCRP (Breast Cancer Resistance Protein, ABCG2) is one of the core efflux transporters identified in FDA and EMA drug-drug interaction guidance, expressed in the intestine, liver, kidney and blood-brain barrier.
The vesicle-based assay uses estrone-3-sulfate as a probe substrate to quantify BCRP-mediated transport into inside-out membrane vesicles, in the presence and absence of test compounds, allowing determination of inhibition potency and IC50 values.
BCRP inhibition can elevate systemic exposure to co-administered substrates, alter brain penetration of CNS-targeted compounds, and is routinely assessed as part of the standard regulatory DDI transporter panel. Because BCRP works alongside P-gp in limiting drug absorption and distribution, many DDI study designs assess both transporters together to capture the full efflux risk profile.
Typical applications
- Drug-induced liver injury (DILI) risk assessment
- Drug-drug interaction (DDI) studies per FDA/EMA guidance
- Hepatotoxicity screening in lead optimisation
- IC50 determination for BCRP inhibitors
- Regulatory transporter panels (BSEP, BCRP, P-gp, MRP1-5, MRP8)
- Academic and pharmaceutical DMPK research
Product information
- Product type: Human BCRP Vesicle Kit
- Source: HEK293-derived inside-out membrane vesicles
- Kit size: 100 reactions (96-well plate format)
- Substrate: Estrone-3-sulfate
- Storage: −80 °C
- Shipment: Dry ice
Available on request
- Certificate of Analysis (CoA)
- Technical data sheet
- Assay protocol support
- Full ABC transporter panel quote
- Bulk order options
Need a complete ABC transporter panel?
Contact our team for BSEP, BCRP, P-gp and MRP kit pricing, technical documentation and assay support for your DMPK study.
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