Description
Product Overview
The Human MRP8 Vesicle Kit (HEK293) provides ready-to-use inside-out membrane vesicles overexpressing human MRP8 (ABCC11) for ATP-dependent vesicular transport studies. MRP8 transports a distinctive substrate profile including steroid sulfates (DHEAS, estrone-3-sulfate), monoanionic bile acids, cAMP, and nucleoside monophosphate analogues. Its expression in mammary gland, brain, liver, and testes makes it relevant in breast cancer DDI research, CNS drug distribution studies, and metabolic profiling of steroid conjugates.
Guaranteed ATP/AMP transport ratio >5 per lot. Use alongside the Human Control Vesicle Kit for matched background subtraction — required for regulatory-grade DDI data per FDA DDI Guidance (2020) and EMA DDI Guideline (2013/2022). Mouse and rat MRP8 isoforms are available on request.
Transporter Profile
| Property | Detail |
|---|---|
| Transporter name | MRP8 — Multidrug Resistance-Associated Protein 8 |
| Gene | ABCC11 |
| Protein family | ABC transporter, ABCC subfamily |
| Tissue expression | Mammary gland, brain, liver, testes, small intestine |
| Key substrates | DHEAS, estrone-3-sulfate (E1S), LTC₄, cAMP, monoanionic bile acids, nucleoside monophosphate analogues |
| Inhibitors (reference) | MK571, probenecid, benzbromarone |
| DDI relevance | Breast cancer drug development, steroid hormone DDI, CNS drug distribution, nucleoside analogue metabolism |
Technical Specifications
| Parameter | Specification |
|---|---|
| Transporter | Human MRP8 (ABCC11) |
| Expression system | HEK293 (transient overexpression) |
| Vesicle type | Inside-out membrane vesicles |
| Reactions per kit | 100 |
| ATP/AMP transport ratio | >5 (guaranteed per lot) |
| 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) |
| Distributor DACH | SeamlessBio GmbH, Passau |
| Regulatory | Research Use Only (RUO) |
Applications
| Application | Description |
|---|---|
| Steroid sulfate efflux studies | Characterise ATP-dependent transport of DHEAS, estrone-3-sulfate (E1S), and other steroid sulfate conjugates — relevant for understanding hormonal drug distribution, steroid metabolite efflux in breast tissue, and endocrine DDI profiling. |
| Breast cancer / mammary tissue DDI | MRP8 is expressed in mammary gland and mediates efflux of steroid hormones and certain anticancer drugs. Use in breast cancer drug development to characterise MRP8-mediated transport of cytotoxics and hormonal therapies, and to assess inhibition potential of investigational compounds. |
| CNS drug distribution | MRP8 expression in brain tissue may restrict CNS exposure of steroid sulfate conjugates and other substrates. Relevant for drugs targeting the CNS where active efflux at brain barriers may limit exposure. |
| Bile acid and hepatic transport | MRP8 transports monoanionic bile acids — relevant in hepatic cholestatic studies alongside BSEP and MRP2, and for compounds subject to enterohepatic cycling of bile acid conjugates. |
| Nucleoside analogue transport | MRP8 effluxes nucleoside monophosphate analogues — relevant for antiviral and anticancer nucleoside analogue drugs where intracellular accumulation and efflux kinetics determine efficacy. |
Assay Principle
Inside-out membrane vesicles present the cytoplasmic face of MRP8 to the external assay buffer, allowing ATP-dependent substrate uptake into the vesicle lumen. Vesicles are incubated with test compound and probe substrate in the presence of ATP (active transport condition) or AMP (background control). The reaction is stopped with cold wash buffer; vesicles are separated by rapid filtration and intravesicular substrate is quantified by LC-MS/MS or radiolabel. The ATP/AMP uptake ratio — calculated against matched Human Control Vesicles — provides the assay window for IC₅₀ determination and substrate classification.
Complete Cell4Pharma Kit Portfolio
Order all ABC transporter vesicle kits from a single EU source — fast cold-chain delivery, guaranteed ATP/AMP ratios, full lot 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 P-gp Vesicle Kit | P-gp / MDR1 | ABCB1 | >5 |
| Human P-gp + FluoPgp Kit | P-gp / MDR1 | ABCB1 | >5 |
| Human Control Vesicle Kit | — | HEK293 empty vector | — |
Available Formats
| Format | Reactions |
|---|---|
| Kit | 100 reactions |
Key Benefits
Batch Reservation
Reserve validated lots up to 36 months for reproducible long-term DDI study workflows.
Full Documentation
Lot-specific QC report and data sheet included with every kit — from ISO 9001 and ISO 13485 certified partner facilities.
EU & Swiss Supply
Manufactured by Cell4Pharma (Netherlands) — fast cold-chain delivery across EU, UK and Switzerland.
Frequently Asked Questions
What substrates and inhibitors are used in the Human MRP8 Vesicle Kit assay?
The standard probe substrates for MRP8 (ABCC11) vesicular transport assays are DHEAS (dehydroepiandrosterone-3-sulfate) and estrone-3-sulfate (E1S), both steroid sulfate conjugates that are well-characterised MRP8 substrates. LTC₄ (leukotriene C₄) and cAMP can also serve as probe substrates. For inhibition studies, reference inhibitors include MK571 (pan-MRP inhibitor), probenecid, and benzbromarone. The Cell4Pharma kit protocol provides lot-specific recommendations for probe substrate concentration and incubation conditions to achieve the guaranteed ATP/AMP ratio of >5.
When should the Human MRP8 Vesicle Kit be included in a DDI transporter panel?
MRP8 (ABCC11) is not currently listed as a primary DDI transporter in FDA (2020) or EMA (2022) guidance, but it is included in extended transporter panels for several specific drug classes. It is particularly relevant when the investigational compound is a steroid sulfate conjugate, a nucleoside monophosphate analogue (e.g. antiviral or anticancer nucleosides), or a compound targeting breast tissue or the CNS where MRP8 expression may affect drug distribution. MRP8 is also studied in the context of earwax type genetics (ABCC11 SNP rs17822931), where variant carriers show altered MRP8 activity — relevant for pharmacogenomics studies.
What is the relationship between MRP8 (ABCC11) and breast cancer drug development?
MRP8 is expressed in mammary gland epithelium and has been studied as a potential mediator of drug efflux in breast tissue. It transports steroid sulfates and certain anticancer drugs, and its expression level has been associated with resistance to some nucleoside analogue-based chemotherapy regimens. In breast cancer drug development, characterising whether an investigational compound is an MRP8 substrate or inhibitor — using vesicular transport assays with the MRP8 Vesicle Kit — informs DDI risk assessment and helps explain tissue-specific distribution or resistance phenotypes.
Are mouse and rat MRP8 isoforms available for species comparison studies?
Yes — mouse and rat MRP8 (ABCC11) isoforms are available on request from Cell4Pharma. Species comparison studies between human, mouse, and rat MRP8 are relevant because rodent and human ABCC11 show differences in substrate selectivity and tissue expression patterns, which can affect the translatability of preclinical in vitro transport data to human DDI prediction. Please contact us with your required isoform, volume, and timeline to confirm availability and lead times.
What documentation is supplied with the Human MRP8 Vesicle Kit?
Every kit shipment includes a lot-specific QC report confirming the ATP/AMP transport ratio (>5) and vesicle preparation parameters, and a data sheet with recommended assay conditions, probe substrates, and reference inhibitor concentrations. All Cell4Pharma kits are manufactured under ISO 9001 and ISO 13485 certified quality systems. Batch reservation for up to 36 months is available on request — important for multi-transporter DDI panels where lot-to-lot consistency between the MRP8 kit and matched Control Vesicle Kit must be maintained across the full study duration.
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