Human MRP1 Vesicle Kit
HEK293-derived inside-out membrane vesicles for MRP1 inhibition screening and drug-drug interaction (DDI) risk assessment, in line with FDA and EMA testing recommendations.
Broad Tissue Distribution
Relevant to systemic disposition and oncology drug resistance, beyond hepatic-specific transporters.
Inside-Out Vesicles
HEK293-derived membrane vesicles with confirmed MRP1 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 MRP1 testing matters in DMPK programs
MRP1 (Multidrug Resistance Protein 1, ABCC1) is a broadly expressed basolateral efflux transporter found in most tissues, with particular relevance in the blood-brain barrier and lung.
The vesicle-based assay uses estradiol-17β-glucuronide as a probe substrate to quantify MRP1-mediated transport into inside-out membrane vesicles, in the presence and absence of test compounds, allowing determination of inhibition potency and IC50 values.
MRP1 inhibition is assessed where compounds are substrates of glutathione- or glucuronide-conjugated efflux, and is relevant to drug resistance mechanisms in oncology programs. Unlike the hepatobiliary-focused MRP2-4, MRP1 has its primary relevance in systemic drug disposition rather than hepatic excretion specifically.
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 MRP1 inhibitors
- Regulatory transporter panels (BSEP, BCRP, P-gp, MRP1-5, MRP8)
- Academic and pharmaceutical DMPK research
Product information
- Product type: Human MRP1 Vesicle Kit
- Source: HEK293-derived inside-out membrane vesicles
- Kit size: 100 reactions (96-well plate format)
- Substrate: Estradiol-17β-glucuronide
- 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
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