Beschreibung
MRP2 (ABCC2) is co-expressed with BSEP at the hepatocyte canalicular membrane and mediates biliary excretion of glucuronide, sulfate, and glutathione conjugates. EMA recommends MRP2 characterisation for compounds undergoing significant hepatic glucuronidation or sulfation.
Human MRP2 Vesicle Kit – Inside-Out Membrane Vesicles for Biliary Drug Excretion and DDI Studies
The Human MRP2 Vesicle Kit (HEK293-derived) from Cell4Pharma provides ready-to-use inside-out membrane vesicles for ATP-dependent transport studies of MRP2 (ABCC2). With a guaranteed ATP/AMP ratio of >20 — the highest in the Cell4Pharma vesicle kit range — this kit delivers exceptional assay sensitivity for IC₅₀ determination and substrate identification. Available exclusively in DACH through SeamlessBio, Passau.
Transporter Profile
MRP2 (ABCC2) is expressed at the canalicular membrane of hepatocytes, brush-border membrane of renal proximal tubules, and intestinal epithelium. It mediates ATP-dependent export of glucuronide, sulfate, and glutathione conjugates into bile and urine. Key substrates: E217βG, GSSG, methotrexate, irinotecan (SN-38-glucuronide), pravastatin. Known inhibitors: MK-571, cyclosporine A, probenecid.
Technische Daten
| Parameter | Spezifikation |
|---|---|
| Transporter | Human MRP2 (ABCC2) |
| Expressionssystem | HEK293 (transient overexpression) |
| Vesicle type | Inside-out membrane vesicles |
| Reaktionen pro Kit | 100 |
| ATP/AMP transport ratio | >20 (highest in range) |
| Detection compatibility | Radiolabel (³H-E217βG), LC-MS/MS |
| Lagerung | −80 °C (supplied on dry ice) |
| Kit contents | Vesicles, ATP, AMP, reaction buffer, wash buffer, CoA |
| Manufacturer | Cell4Pharma (Netherlands) |
| DACH-Vertriebspartner | SeamlessBio GmbH, Passau, Germany |
Anwendungen
| Anwendung | Description |
|---|---|
| Biliary drug excretion profiling | Quantify MRP2-mediated hepatic canalicular efflux of glucuronide/sulfate conjugates — essential for biliary clearance prediction and enterohepatic circulation studies. |
| EMA-recommended DDI assessment | EMA 2022 guideline recommends MRP2 characterisation for compounds with significant hepatic glucuronidation or sulfation. IC₅₀ data from vesicle assays is accepted. |
| Renal tubular efflux studies | MRP2 in renal proximal tubules contributes to urinary excretion of phase II metabolites. |
| Enterohepatic recycling studies | MRP2 in intestinal epithelium shapes enterohepatic circulation of glucuronidated drugs. |
Assay Principle
Inside-out membrane vesicles present the cytoplasmic face of the transporter to the assay buffer, enabling ATP-dependent substrate uptake into the vesicle lumen. Incubate with test compound and probe substrate in the presence of ATP (transport) or AMP (background). Stop with cold wash buffer, filter vesicles, and quantify by LC-MS/MS or radiolabel. The ATP/AMP ratio of >20 provides an exceptional assay window for reliable IC₅₀ curves.
Key Benefits
Highest ATP/AMP Ratio
ATP/AMP >20 — the widest assay window in the Cell4Pharma range for MRP2.
Vollständige Dokumentation
Lot-specific QC report, data sheet, CoA included with every kit.
EU Stock
Warehoused in Passau, Germany — fast cold-chain delivery across EU, UK and Switzerland.
Häufig gestellte Fragen
Why does MRP2 have the highest ATP/AMP ratio (>20)?
The high ratio reflects MRP2’s exceptional active transport efficiency. It means a wider assay window, lower compound concentrations needed to detect inhibition, more reliable IC₅₀ curves, and higher-confidence data for regulatory submissions.
Is MRP2 required in the FDA DDI submission package?
FDA does not list MRP2 as a mandatory Tier 1 transporter, but EMA recommends it for compounds with significant glucuronidation. For full regulatory coverage across both agencies, MRP2 data is valuable.
Can MRP2 be ordered together with BSEP?
Yes — both are canalicular transporters and are frequently profiled together. SeamlessBio supplies BSEP and MRP2 kits from the same EU stock with combined cold-chain shipment.
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