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Corning® Gentest? Vesicle Assay Kits

Corning® Gentest? Vesicle Assay Kits
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Corning® Gentest? Vesicle Assay Kits - 1

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 Supports FDA-recommended BCRP, and EMA- recommended BSEP, as well as MRP vesicle panel w Provides two simple protocols to accommodate human and animal ABC transporter vesicle studies; one for MRP/BCRP and one for BSEP w Delivers maximum flexibility allowing researchers the ability to perform a single transporter study or both MRP and BCRP studies with one kit w Supports high-volume cell harvester applications with bulk wash buffers available separately (10X wash buffer for MRP/BCRP and 10X wash buffer for BSEP) w Provides researchers an alternative to radiolabeled compounds with included CDCF fluorescent substrate for MRP2/MRP3 transporters w Saves researchers time by eliminating reagent preparation steps; assays can be completed within one day w Supports 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) European Medicines Agency: Guideline on the Investigation of Drug Interactions, DRAFT, April 2010

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Corning® Gentest? Vesicle Assay Kits - 2

Vesicle Kit Lot-to-Lot Variance for MRP2, BCRP, and BSEP Ordering Information Corning® Gentest™ MRP/BCRP Vesicle Assay Kit Kit contains reagents for 200 assays Assay Uptake Buffer; 10X Wash Buffer; 200 mM ATP; 200 mM AMP; 300mM GSH; MRP3 Substrate BCRP Substrate MRP2/MRP3 Fluorescent Substrate MRP1/MRP2 Substrate Corning Gentest BSEP Vesicle Assay Kit Kit contains reagents for 200 assays Assay Uptake Buffer; 10X Wash Buffer; 200 mM ATP; 200 mM AMP; BSEP Substrate; Blocking Buffer (50X) Corning Gentest 10X Wash Buffers Cat. No. 1.1. ignal minus noise (ATP-dependent uptake activity) S...

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