Human P-gp Vesicle Kit
HEK293-derived inside-out membrane vesicles for P-gp inhibition screening and drug-drug interaction (DDI) risk assessment, in line with FDA and EMA testing recommendations.
Most Widely Tested Transporter
Near-universal requirement in regulatory DDI packages due to broad tissue distribution and substrate overlap.
Inside-Out Vesicles
HEK293-derived membrane vesicles with confirmed P-gp expression and inside-out orientation for reliable, reproducible transport data.
100 Reactions per Kit
Each kit is sized for 100 reactions based on a 96-well plate format, suitable for IC50 determination and single-concentration screening.
Dry Ice Shipment
Shipped frozen at −80 °C on dry ice to preserve vesicle integrity and transport activity upon arrival.
Why P-gp testing matters in DMPK programs
P-glycoprotein (P-gp, ABCB1) is the most extensively characterised efflux transporter in drug development, expressed at the intestinal brush border, blood-brain barrier, liver and kidney.
The vesicle-based assay uses N-methyl-quinidine (NMQ) or digoxin as a probe substrate to quantify P-gp-mediated transport into inside-out membrane vesicles, in the presence and absence of test compounds, allowing determination of inhibition potency and IC50 values.
P-gp inhibition can substantially increase oral bioavailability and brain penetration of co-administered substrates, making it a near-universal component of regulatory DDI assessment for new chemical entities. P-gp is frequently assessed together with BCRP, since both transporters share overlapping substrate specificity and jointly determine intestinal and blood-brain barrier efflux.
Typical applications
- Drug-induced liver injury (DILI) risk assessment
- Drug-drug interaction (DDI) studies per FDA/EMA guidance
- Hepatotoxicity screening in lead optimisation
- IC50 determination for P-gp inhibitors
- Regulatory transporter panels (BSEP, BCRP, P-gp, MRP1-5, MRP8)
- Academic and pharmaceutical DMPK research
Product information
- Product type: Human P-gp Vesicle Kit
- Source: HEK293-derived inside-out membrane vesicles
- Kit size: 100 reactions (96-well plate format)
- Substrate: N-methyl-quinidine (NMQ) or digoxin
- Storage: −80 °C
- Shipment: Dry ice
Available on request
- Certificate of Analysis (CoA)
- Technical data sheet
- Assay protocol support
- Full ABC transporter panel quote
- Bulk order options
Need a complete ABC transporter panel?
Contact our team for BSEP, BCRP, P-gp and MRP kit pricing, technical documentation and assay support for your DMPK study.
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