Human Pgp vesicle kit (HEK293 derived) C4PVK010
Human Pgp vesicle kit (HEK293 derived) C4PVK010

Human Pgp Vesicle Kit (HEK293-derived)

Detailed Overview of the Human Pgp Vesicle Kit The Human Pgp Vesicle Kit provides inside-out membrane vesicles...
Vendor: Cell4Pharma
SKU: C4PVK010
Availability: In stock
€1.450,00
€1.450,00
Test: 100
Subtotal: €1.450,00
Human Pgp vesicle kit (HEK293 derived) C4PVK010

Human Pgp Vesicle Kit (HEK293-derived)

€1.450,00
Human Pgp vesicle kit (HEK293 derived) C4PVK010

Human Pgp Vesicle Kit (HEK293-derived)

€1.450,00
Test: 100
Description
Description
x

Detailed Overview of the Human Pgp Vesicle Kit

The Human Pgp Vesicle Kit provides inside-out membrane vesicles isolated from HEK293 cells transiently overexpressing P-glycoprotein (P-gp / MDR1 / ABCB1). P-gp is one of the most clinically relevant drug efflux transporters and is present at key pharmacokinetic barriers including the intestine, liver, kidney, and blood-brain barrier. The kit is compliant with FDA (2017) and EMA (2013) DDI guidance.

Manufactured by Cell4Pharma. A variant with the novel fluorescent FluoPgp substrate is also available (C4PVK011). 
Available exclusively in the D-A-CH region via SeamlessBio.

Transporter Profile 

Name: P-gp, P-glycoprotein, MDR1, Multidrug resistance protein 1, Permeability glycoprotein, ABCB1, ATP-binding cassette sub-family B member 1
Gene: ABCB1
ATP/AMP ratio: >5 (guaranteed)

Tissue expression:  Intestine, liver, kidney, blood-brain barrier, many tumor cells

Known substrates: Convallatoxin, digoxin, N-methyl-quinidine (NMQ), colchicine, tacrolimus, quinidine, etoposide, doxorubicin

In stock: Human Pgp. Also available: mouse and rat Pgp

Kit Contents (100 Reactions)

  • Vesicle vial (100 reactions),Pgp-overexpressing HEK293-derived
  • AMP-ATP solution (100 mM), Cell4Pharma
  • Assay buffer, Cell4Pharma
Note: C4PVK011 additionally contains the novel FluoPgp fluorescent substrate for fluorescence-based detection without radiolabeling.

Applications

  • P-gp substrate identification and efflux characterization
  • Drug-drug interaction (DDI) studies per FDA/EMA guidance
  • Multidrug resistance (MDR) mechanism studies
  • Blood-brain barrier penetration assessment (in vitro)
  • Inhibition studies and IC50 determination
  • High-throughput screening (radiolabel, fluorescent, LC-MS detection)

Regulatory Compliance

P-glycoprotein (ABCB1) is a primary transporter listed in FDA (2017) and EMA (2013) DDI guidelines. Evaluation of P-gp substrate and inhibitor status is required for all new molecular entities (NMEs) with significant oral or systemic exposure entering clinical development.

Technical Specifications

Host cell: HEK293 (human embryonic kidney)

Vesicle type:Inside-out membrane vesicles

Format: 100 reactions per kit
Detection:Radiolabel / fluorescent / LC-MS compatibleVariant with FluoPgp
substrate: C4PVK011
Storage: –80 °C

Cross-References & Related Products

  • Human Pgp Vesicle Kit + FluoPgp Substrate (C4PVK011) – fluorescent detection variant, no radiolabeling required
  • Human BCRP Vesicle Kit (C4PVK006) – for parallel BCRP efflux assessment
  • Human Control Vesicle Kit (C4PVK009) – recommended as negative control
  • ciPTEC-OAT1 Assay-Ready Cells – express functional endogenous P-gp (ABCB1) for cell-based confirmatory studies
  • Human Serum AB Male OTC (SeamlessBio) – for ciPTEC culture medium supplementation
All products available on request.
Contact: info@seamlessbio.de | Phone: +49 851 37932226

Datasheet


Publication

Gozalpour E, Wittgen HG, van den Heuvel JJ, et al. Interaction of digitalis-like compounds with p-glycoprotein. Toxicol Sci. 2013,131(2):502-11. doi: 10.1093/toxsci/kfs307 

Introduction to the Human Pgp Vesicle Kit

The Human Pgp Vesicle Kit (HEK293-derived) is designed to offer researchers a highly specific tool for studying P-glycoprotein (Pgp) function in vitro. Derived from HEK293 cells, this kit provides membrane vesicles enriched with functional human Pgp, allowing for precise evaluation of drug-transporter interactions. It supports various applications, including drug screening and pharmacokinetic profiling, delivering consistent and reproducible results. Utilizing this kit saves time and improves data reliability in assessing drug efflux mechanisms relevant to multidrug resistance.

Key Features and Benefits

This Human Pgp Vesicle Kit stands out due to its high purity and functional integrity of Pgp vesicles derived from HEK293 cells. The vesicles maintain optimal transporter activity, making them ideal for substrate and inhibitor screening assays. The kit includes all necessary reagents and detailed protocols to streamline assay setup. Its robust design ensures minimal batch-to-batch variability, providing dependable data. Researchers benefit from a user-friendly format that accelerates assay development and supports drug discovery projects targeting Pgp-mediated transport.

Applications in Drug Discovery and Research

The Human Pgp Vesicle Kit is widely used for evaluating drug-transporter interactions, crucial in understanding drug absorption, distribution, and resistance. Its application extends to screening compounds for Pgp inhibition or substrate potential, aiding in predicting drug-drug interactions and toxicology. The kit is also suitable for mechanistic studies on Pgp function, offering insights into transporter kinetics. Due to its HEK293 origin, the vesicles closely mimic human Pgp activity, making it a valuable asset in pharmaceutical research and early-stage drug development.

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