Corning® Gentest? Vesicle Assay Kits0 pages
Corning® Gentest™ Vesicle Assay Kits
MRP/BCRP and BSEP Reagent Kits for ABC Transporter
Vesicle Assays
The Corning Gentest vesicle assay kits are flexible,
complete reagent kits delivering consistency across
lots for testing all Corning human and animal ABC
transporter vesicles with two simple protocols; one
for MRP/BCRP and one for BSEP, and aligned with
industry guidance recommendations.
Features
w tSupports FDA-recommended BCRP, and EMA-
recommended BSEP, as well as MRP vesicle panel
w tProvides two simple protocols to accommodate
human and animal ABC transporter vesicle
studies; one for MRP/BCRP and one for BSEP
w tDelivers maximum flexibility allowing
researchers the ability to perform a single
transporter study or both MRP and BCRP studies
with one kit
w tSupports high-volume cell harvester applications
with bulk wash buffers available separately (10X
wash buffer for MRP/BCRP and 10X wash buffer
for BSEP)
w tProvides researchers an alternative to
radiolabeled compounds with included
CDCF fluorescent substrate for MRP2/MRP3
transporters
w tSaves researchers time by eliminating reagent
preparation steps; assays can be completed
within one day
w tSupports multiple time usage with robust, stable
reagents accommodating up to six freeze-thaw
cycles
Kit supports industry guidance recommendations for ABC
transporters
The kit supports International Transporter Consortium (ITC)1 and
European Medicines Agency (EMA)2 recommended BCRP and BSEP
in vitro transporter studies. ATP, AMP, and other essential reagents
included in this kit are aligned with the ITC transporter white paper
published in March 2010.1
Physiological, well documented substrates were selected for
easy literature comparison when determining whether a new
chemical entity (NCE) is a substrate or inhibitor of BCRP, MRP, or
BSEP: Estrone-3-Sulfate (BCRP substrate), Leukotriene C4 (MRP1/
MRP2 substrate), Estradiol-17b-D-Glucuronide (MRP3 substrate),
Taurocholic Acid (BSEP substrate).
Fluorescent substrate for MRP2/MRP3 vesicle provides an
alternative to radiolabeled compounds
CDCF (5(6)-carboxy-2’,7’-dichlorofluorescein) is a well-characterized
fluorescent substrate for MRP2/MRP3. Using CDCF to identify
MRP2 and MRP3 inhibitors eliminates the need for radiolabeled
compounds and the waste removal and radiation license requirements associated with their use.
Provides a high degree of reagent lot-to-lot consistency
Three MRP/BCRP and three BSEP kit lots were evaluated for lot-tolot consistency using the same hMRP2, hBCRP, and hBSEP vesicle
lots and the results obtained demonstrated reproducibility within
experimental uncertainty (see Figure 1/Table 1).
Flexible and stable format with two kits, two protocols for all
Corning human and animal transporter vesicles
Designed for maximum flexibility and researcher convenience, one
vesicle protocol accommodates human and animal BCRP/MRP and
another supports BSEP studies. The kits accommodate up to 200
assays. The stability of both kits were validated for up to six freezethaw cycles with no significant loss in activity (see Figure 2).
1
International Transporter Consortium (ITC) Drug Transporter Guidance Paper, Nature Reviews/Drug
Discovery MARCH 2010 | VOLUME 9 (www.nature.com/reviews/drugdisc)
2
European Medicines Agency: Guideline on the Investigation of Drug Interactions, DRAFT, April 2010
"