Description
MRP5 (ABCC5) is unique among the MRP family for its ubiquitous tissue expression — heart, brain, skeletal muscle, testis and more. It transports cyclic nucleotides (cAMP, cGMP), nucleoside monophosphate analogues, and organic anions, making it especially relevant for antiviral and anticancer nucleoside analogue drugs.
Human MRP5 Vesicle Kit – Inside-Out Membrane Vesicles for Ubiquitous Organic Anion and Cyclic Nucleotide Transport Studies
The Human MRP5 Vesicle Kit (HEK293-derived) from Cell4Pharma provides ready-to-use inside-out membrane vesicles for ATP-dependent transport studies of MRP5 (ABCC5). Unlike other MRPs with organ-specific expression, MRP5 is ubiquitously expressed and handles cyclic nucleotides, nucleotide analogues, and organic anions. Each kit delivers 100 reactions with a guaranteed ATP/AMP ratio of >5. Available in DACH exclusively through SeamlessBio, Passau.
Transporter Profile
MRP5 (ABCC5) is ubiquitously expressed in heart, brain, skeletal muscle, testes, and many other tissues. It transports cyclic nucleotides (cAMP, cGMP), organic anions, glutathione conjugates, and nucleoside monophosphate analogues. Key substrates: cAMP, cGMP, PMEA, fluorescein. Its broad distribution means MRP5 inhibition can potentially affect drug distribution across multiple tissue compartments.
Technical Specifications
| Parameter | Specification |
|---|---|
| Transporter | Human MRP5 (ABCC5) |
| Expression system | HEK293 (transient overexpression) |
| Vesicle type | Inside-out membrane vesicles |
| Reactions per kit | 100 |
| ATP/AMP transport ratio | >5 |
| Detection compatibility | Radiolabel, LC-MS/MS |
| Storage | −80 °C (supplied on dry ice) |
| Kit contents | Vesicles, ATP, AMP, reaction buffer, wash buffer, CoA |
| Manufacturer | Cell4Pharma (Netherlands) |
| DACH Distributor | SeamlessBio GmbH, Passau, Germany |
Applications
| Application | Description |
|---|---|
| Nucleoside analogue transport profiling | Screen anticancer and antiviral nucleoside monophosphate analogues as MRP5 substrates — relevant for intracellular drug accumulation and resistance mechanisms. |
| CNS drug distribution | MRP5 at the blood-brain barrier may restrict CNS penetration of organic anions — relevant for CNS drug development programs. |
| Broad tissue distribution profiling | Characterise MRP5-mediated efflux in cardiac, testicular, and CNS compartments where ubiquitous expression is pharmacologically relevant. |
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 provides the assay window for IC₅₀ determination.
Key Benefits
Ubiquitous Expression
Only MRP kit covering CNS, cardiac, and testicular distribution in a single assay system.
Full Documentation
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.
Frequently Asked Questions
How does MRP5 differ from MRP4 in substrate selectivity?
MRP4 and MRP5 share some substrates (cAMP, cGMP, PMEA) but differ in expression patterns. MRP4 is more renal-dominant; MRP5 is ubiquitous with notable CNS/cardiac expression. Running both kits in parallel provides comprehensive nucleotide analogue profiling.
Is MRP5 a regulatory requirement?
MRP5 is not a Tier 1 regulatory requirement, but is increasingly included in comprehensive DDI packages for antiviral and anticancer nucleoside analogues, particularly for CNS-targeted compounds.
Can MRP5 be ordered together with MRP4?
Yes — SeamlessBio supplies the complete Cell4Pharma MRP kit range from EU stock. Combined cold-chain shipment available for MRP4 + MRP5 and any other kit combination.
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