Vesicular Transport Assays

Service Cell Line Transporter Technology Membrane Type Probe Substrate Read Out Reference Inhibitor Positive Control Dynamic Range
Bcrp- Cynomolgus monkey Vesicular Transporter Assay Bcrp - cynomolgus monkey
Vesicular Transport Assay
Estrone 3-sulfate Ko143
BCRP Vesicular Transport Assay - Estrone 3-sulfate BCRP
Vesicular Transport Assay
Estrone 3-sulfate Ko143
BCRP Vesicular Transport Assay - MTX BCRP
Vesicular Transport Assay
Methotrexate (MTX) Ko143
BCRP Vesicular Transport Assay - Rosuvastatin BCRP
Vesicular Transport Assay
Rosuvastatin Ko143
BCRP Vesicular Transport Assay - Uric acid BCRP
Vesicular Transport Assay
Uric acid Ko143
Bcrp1- Mouse Vesicular Transport Assay Bcrp - mouse
Vesicular Transport Assay
Estrone 3-sulfate Ko143
Bsep- Cynomolgus monkey Vesicular Transporter Assay Bsep - cynomolgus monkey
Vesicular Transport Assay
Taurocholic acid Cyclosporin A
Bsep- Dog Vesicular Transporter Assay Bsep - dog
Vesicular Transport Assay
Taurocholic acid Cyclosporin A
Bsep- Mouse Vesicular Transport Assay Bsep - mouse
Vesicular Transport Assay
Taurocholic acid Cyclosporin A
Bsep- Rat Vesicular Transport Assay Bsep - rat
Vesicular Transport Assay
Taurocholic acid Cyclosporin A
BSEP Vesicular Transport Assay BSEP
Vesicular Transport Assay
Taurocholic acid Cyclosporin A
Mdr1- Cynomolgus monkey Vesicular Transporter Assay Mdr1 - cynomolgus monkey
Vesicular Transport Assay
NMQ Valspodar
MDR1/P-gp Vesicular Transport Assay MDR1/P-gp
Vesicular Transport Assay
N-methyl-quinidine (NMQ) Valspodar, Verapamil
Mdr1a- Mouse Vesicular Transport Assay Mdr1a - mouse
Vesicular Transport Assay
NMQ Cyclosporin A
MRP1 Vesicular Transport Assay - Leukotriene C4 MRP1
Vesicular Transport Assay
Leukotriene C4 MK-571
MRP1 Vesicular Transport Assay - β-Estradiol 17-(β-D-glucuronide) MRP1
Vesicular Transport Assay
β-Estradiol 17-(β-D-glucuronide) Benzbromarone
Mrp2 - Rat Vesicular Transport Assay Mrp2 - rat
Vesicular Transport Assay
β-Estradiol 17-(β-D-glucuronide) Benzbromarone
MRP2 Vesicular Transport Assay - Coproporphyrin I MRP2
Vesicular Transport Assay
Coproporphyrin I Benzbromarone
MRP2 Vesicular Transport Assay - β-Estradiol 17-(β-D-glucuronide) MRP2
Vesicular Transport Assay
β-Estradiol 17-(β-D-glucuronide) Benzbromarone
MRP3 Vesicular Transport Assay MRP3
Vesicular Transport Assay
β-Estradiol 17-(β-D-glucuronide) MK-571, Benzbromarone
MRP4 Vesicular Transport Assay MRP4
Vesicular Transport Assay
DHEAS MK-571
MRP5 Vesicular Transport Assay MRP5
Vesicular Transport Assay
CDCF Benzbromarone
Mdr1b- Rat Vesicular Transport Assay Mdr1b - rat
Vesicular Transport Assay
NMQ Verapamil
Mrp3- Rat Vesicular Transport Assay Mrp3 - rat
Vesicular Transport Assay
β-Estradiol 17-(β-D-glucuronide) MK-571

Description

The vesicular transport assay is performed using inside out vesicles from membranes expressing the transporter of interest. The method can be applied to measure either inhibitory or substrate type interactions with ABC efflux transporters. The vesicular transport inhibition assay is a robust and quick assay suitable for screening large numbers of compounds. The read-out of the assay is easy to interpret and suitable for IC50 determinations (ITC reference ). The success of substrate assays depends very much on the passive permeability of the compound. High permeability compounds will diffuse out of the vesicles and therefore will not be detected as substrates.

SOLVO Biotechnology offers vesicular transport substrates studies in four levels. The launch of the given Part(s) depend(s) on the success of the previous Part(s).

Part 1 – Vesicular Transport inhibitor assessment (IC50 determination)

Part 2.1. – Vesicular Transport substrate assessment - feasibility studies: pilot experiments to determine the feasibility of testing

Part 2.2. – Vesicular Transport substrate assessment - characterization studies: Detailed characterization of the transport, determination of KM and Vmax

Part 2.3. – Optional Part for characterizing potential drug-drug interactions

Advantages of the Vesicular Transport Assay

Inhibition analysis suitable for any type of compound concerning its permeability
• Uptake measurements for low to medium permeability compounds
• Quick and easy
• Modelling of IC50 concentration
• Vesicles can be prepared from any cell type
• Large dynamic range
• Flexible readout (LSc, Fluo, LC/MS)

Learn more about the Technology background of the Vesicular Transport Assay

For each of the Vesicular Transport Assays listed above characterization files with more information about the performance of the assay are available. Characterization files describe the time-linearity course for a given probe substrate, the concentration dependent kinetics (Km/Vmax) determined and IC50 values generated for selected inhibitors. To request this information please contact your local Business Development representative directly or send a general inquiry to .(JavaScript must be enabled to view this email address).