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The Human MRP2 Vesicle Kit (HEK293 derived) provides ready-to-use inside-out membrane vesicles for ATP-dependent transport studies of Multidrug Resistance-Associated Protein 2 (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. MRP2 is co-expressed with BSEP at the hepatocyte canalicular membrane and is a key determinant of biliary drug excretion.
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. EMA recommends MRP2 investigation for compounds that undergo significant glucuronidation or sulfation. Key substrates: E217βG, GSSG, methotrexate, irinotecan (SN-38-glucuronide), pravastatin. Known inhibitors: MK-571, cyclosporine A, probenecid.
| Parameter | Specification |
|---|---|
| Transporter | Human MRP2 (Multidrug Resistance-Associated Protein 2) (ABCC2) |
| Expression system | HEK293 (transient overexpression) |
| Vesicle type | Inside-out membrane vesicles |
| Reactions per kit | 100 |
| ATP/AMP transport ratio | >20 |
| Detection compatibility | Radiolabel (³H-E217βG), LC-MS/MS |
| Storage | −80 °C (supplied on dry ice) |
| Kit contents | Vesicles, ATP, AMP, reaction buffer, wash buffer, CoA |
| Manufacturer | Cell4Pharma (Netherlands) |
| Distributor DACH | SeamlessBio GmbH, Passau |
| Application | Description |
|---|---|
| Biliary drug excretion profiling | Quantify MRP2-mediated hepatic canalicular efflux of glucuronide/sulfate drug conjugates — essential for prediction of biliary clearance and enterohepatic circulation. |
| 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. Relevant for renal DDI risk assessment. |
| Enterohepatic recycling studies | MRP2 in intestinal epithelium contributes to enteric efflux and shapes the enterohepatic circulation of glucuronidated drugs. |
Inside-out membrane vesicles present the cytoplasmic face of the transporter to the assay buffer, allowing ATP-dependent substrate uptake into the vesicle lumen. Incubate vesicles with test compound and probe substrate in the presence of ATP (transport) or AMP (background control). Stop reaction with cold wash buffer, separate vesicles by filtration, and quantify accumulated substrate by LC-MS/MS, radiolabel, or fluorescence. The ATP/AMP ratio provides the assay window for reliable IC₅₀ determination.
Order all ABC transporter vesicle kits from a single EU source — fast cold-chain delivery, guaranteed ATP/AMP ratios, full documentation.
| Kit | Transporter | Gene | ATP/AMP Ratio |
|---|---|---|---|
| Human BCRP Vesicle Kit | BCRP | ABCG2 | >10 |
| Human BSEP Vesicle Kit | BSEP | ABCB11 | >10 |
| Human MRP1 Vesicle Kit | MRP1 | ABCC1 | >5 |
| Human MRP2 Vesicle Kit | MRP2 | ABCC2 | >20 |
| Human MRP3 Vesicle Kit | MRP3 | ABCC3 | >5 |
| Human MRP4 Vesicle Kit | MRP4 | ABCC4 | >5 |
| Human MRP5 Vesicle Kit | MRP5 | ABCC5 | >5 |
| Human MRP8 Vesicle Kit | MRP8 | ABCC11 | >5 |
| Human Pgp Vesicle Kit | P-gp / MDR1 | ABCB1 | >5 |
| Human Pgp + FluoPgp Kit | P-gp / MDR1 | ABCB1 | >5 |
| Human Control Vesicle Kit | — | HEK293 empty vector | — |
| Advantage | Description |
|---|---|
| ✅ EU warehouse stock | Fast cold-chain delivery across Germany, Austria, Switzerland and the EU |
| ✅ Direct contact | Speak to a scientist, not a call centre — in German or English |
| ✅ Full documentation | Data sheet, QC report and invoice with every shipment |
| ✅ Batch reservation | Reserve a specific lot for your entire project duration |
| ✅ Complete portfolio | All 11 Cell4Pharma kits from one source — BCRP, BSEP, MRP1–8, Pgp, Control |
Order or request pricing: info@seamlessbio.de | +49 851 37932226
The ATP/AMP ratio reflects the active transport efficiency of the overexpressed transporter relative to passive diffusion. MRP2's very high ratio (>20) means an exceptional assay window — lower compound concentrations required to see inhibition, more reliable IC₅₀ curves, and higher confidence data for regulatory submissions.
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 — particularly for compounds undergoing significant hepatic/intestinal glucuronidation.
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