Beschreibung
MRP1 (ABCC1) is an ATP-binding cassette efflux transporter broadly expressed in lung, testis, kidney, blood-brain barrier, and immune cells. It mediates ATP-dependent export of glutathione conjugates, glucuronides, sulfate conjugates, and anticancer drugs — making it a critical transporter in oncology DDI studies and tissue distribution profiling.
Human MRP1 Vesicle Kit – Inside-Out Membrane Vesicles for Multidrug Resistance and Organic Anion Transport Studies
The Human MRP1 Vesicle Kit (HEK293-derived) from Cell4Pharma provides ready-to-use inside-out membrane vesicles for ATP-dependent transport studies of Multidrug Resistance-Associated Protein 1 (MRP1 / ABCC1). Each kit delivers 100 reactions with a guaranteed ATP/AMP ratio of >5. Available exclusively in DACH through SeamlessBio — fast EU cold-chain delivery from Passau, Germany.
Transporter Profile
MRP1 (ABCC1) is broadly expressed in lung, testis, kidney, blood-brain barrier, cardiac and skeletal muscle, placenta, and macrophages. It transports glutathione (GSH), glutathione conjugates (GS-X), glucuronides, sulfate conjugates, and lipophilic drugs complexed with glutathione. Key substrates: E217βG, GSSG, saquinavir, ritonavir, methotrexate, daunorubicin, leukotrienes. Known inhibitors: MK-571, probenecid, indomethacin.
Technische Daten
| Parameter | Spezifikation |
|---|---|
| Transporter | Human MRP1 (ABCC1) |
| Expressionssystem | HEK293 (transient overexpression) |
| Vesicle type | Inside-out membrane vesicles |
| Reaktionen pro Kit | 100 |
| ATP/AMP transport ratio | >5 |
| Detection compatibility | Radiolabel (³H-E217βG), LC-MS/MS, fluorescence |
| 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 |
|---|---|
| Multidrug resistance (MDR) profiling | Assess whether anticancer compounds are MRP1 substrates — relevant for tumour drug efflux, resistance mechanisms, and combination therapy design. |
| Glutathione/glucuronide conjugate transport | Characterise phase II metabolite efflux via MRP1 — important for systemic exposure of conjugated drug metabolites. |
| Blood-brain barrier distribution | MRP1 at the BBB restricts CNS drug access — relevant for CNS drug candidates. |
| Tissue DDI profiling | Assessment of MRP1-mediated interactions at lung, cardiac, and immune cell sites. |
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, radiolabel, or fluorescence. The ATP/AMP ratio defines the assay window for IC₅₀ determination.
Key Benefits
Sammelreservierung
Reserve validated lots up to 24 months for reproducible long-term workflows.
Vollständige Dokumentation
CoA, QC report, data sheet and additional certificates included with every shipment.
EU Stock
Warehoused in Passau, Germany — fast cold-chain delivery across EU, UK and Switzerland.
Häufig gestellte Fragen
Is MRP1 a regulatory requirement for DDI submissions?
MRP1 is not listed as a mandatory Tier 1 transporter by FDA or EMA, but is recommended for oncology compounds, compounds with significant lung/brain/cardiac distribution, or extensive phase II metabolites.
What probe substrate is recommended for MRP1?
E217βG (estradiol-17β-D-glucuronide) is the standard probe — available as ³H-labelled or unlabelled for LC-MS/MS. GSSG is also commonly used.
Can I order MRP1 together with other MRP kits?
Yes — SeamlessBio supplies the complete Cell4Pharma portfolio (MRP1–8, P-gp, BCRP, BSEP, Control) from a single EU source with combined cold-chain shipment.
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