Human MRP3 Vesicle Kit
HEK293-derived inside-out membrane vesicles for MRP3 inhibition screening and drug-drug interaction (DDI) risk assessment, in line with FDA and EMA testing recommendations.
Compensatory Efflux Pathway
Protective basolateral route activated when canalicular bile acid excretion is impaired.
Inside-Out Vesicles
HEK293-derived membrane vesicles with confirmed MRP3 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 MRP3 testing matters in DMPK programs
MRP3 (ABCC3) is a basolateral hepatic transporter that provides a compensatory route for bile acid and bilirubin efflux back into the bloodstream when canalicular excretion via BSEP or MRP2 is impaired.
The vesicle-based assay uses estradiol-17β-glucuronide as a probe substrate to quantify MRP3-mediated transport into inside-out membrane vesicles, in the presence and absence of test compounds, allowing determination of inhibition potency and IC50 values.
MRP3 upregulation is a known hepatic adaptive response to cholestasis, and its inhibition is assessed to understand whether a compound removes this protective compensatory pathway. A compound that inhibits both BSEP and MRP3 removes both the primary and compensatory bile acid efflux routes, representing a combined risk signal of particular regulatory interest.
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 MRP3 inhibitors
- Regulatory transporter panels (BSEP, BCRP, P-gp, MRP1-5, MRP8)
- Academic and pharmaceutical DMPK research
Product information
- Product type: Human MRP3 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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