High-performance inside-out membrane vesicles for direct evaluation of ATP-dependent P-gp efflux activity.
Description
The Vesitra™ Human P-gp (MDR1) Membrane Vesicles provide a robust, cell-free system to directly measure the ATP-driven extrusion of compounds. By isolating the transport mechanism from cellular uptake and metabolism, this inside-out vesicle model offers a highly specific platform for identifying P-gp substrates and inhibitors with exceptional kinetic clarity.
Brand
Vesitra™
Development Stage
ADME
ADME Research Domain
Excretion
Features
1. Complete isolation of efflux activity free from complex cellular background interference. 2. Robust ATP-dependent transport validated with classic substrates like N-methyl-quinidine. 3. Ideally suited for high-throughput screening and detailed kinetic (Km/Vmax) analysis.
Applications
Rapid screening of P-gp mediated efflux potential; Precise mechanistic determination of drug-drug interactions (DDI) at the efflux pump level.
Species
Human
Expression System
Baculovirus-infected Sf9 insect cells
Physical State
Ready-to-use Suspension
Transporter
P-gp
Gene
ABCB1
Probe Substrate
N-Methylquinidine (NMQ) / Digoxin
Reference Inhibitor
Verapamil / Valspodar
Protein Concentration
5 mg/mL
Total Protein
2.5 mg per vial
Volume
0.5 mL; 1 mL
Vesicle Type
Inside-out ABC Transporter Membrane Vesicles
Background
P-glycoprotein (ABCB1/MDR1) is the most prominent efflux pump in the human body, highly expressed in the intestine, liver, kidney, and blood-brain barrier. It actively protects tissues from xenobiotics and is a primary cause of multidrug resistance.
Shipping
Dry ice
Storage
Store immediately at -80°C upon receipt. Do not store in liquid nitrogen or standard -20°C freezers.
Handling Notes
1. Thaw the vial quickly by gently agitating it in a 37°C water bath (usually takes 1-2 minutes). 2. Immediately place the vial on ice once thawed. 3. Avoid repeated freeze-thaw cycles. If aliquoting is necessary, do so rapidly on ice immediately after the initial thaw, and snap-freeze the aliquots back at -80°C.
Background Control
It is highly recommended to perform assays alongside Mock/Control Vesicles (derived from cells infected with an empty vector) to subtract non-specific background binding.
Batch-to-Batch Consistency
A lot-specific Certificate of Analysis (CoA) is provided with each shipment, documenting the exact ATP-dependent uptake rates (e.g., pmol/mg protein/min).