Corning® Gentest? High Throughput ADME Screening Tools
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Corning® Gentest™ High Throughput ADME Screening Tools Screen for drug-drug interactions, human MDR1 (P-gp) interactions, and metabolic stability Corning Gentest Human P450 Inhibition Screening Kits Screen for drug-drug interactions w Easy to use w Established and validated technology w Complete kit and detailed instruction manual Adverse drug-drug interactions are a major reason drug candidates fail to obtain FDA approval. Many drug-drug interactions are metabolism-based (i.e., two or more drugs competing for metabolism by the same enzyme). The majority of these interactions involve cytochrome P450s. Historically, the discovery of adverse drug interactions has occurred in clinical trials, or after the drug is commercially released. The availability of fluorescent P450 substrates allows high throughput screening for potential P450 inhibitors in the early stages of drug discovery. 120 Furafylline Ketoconazole Sulfaphenazole Tranylcypromine Percent Control Each Corning Gentest P450 High Throughput Inhibitor Screening kit provides all the necessary components and instructions for measuring the IC50 value for up to 38 test compounds in 96 well plates. These kits can accommodate other plate formats (e.g., 384 and 1536 well), with proper scaling. Each inhibitor screening kit includes the following components: recombinant human P450 (Corning Supersomes™ Enzymes), fluorescent P450 substrate, positive control inhibitor, metabolite standard, NADPH regenerating system, reaction buffer, stop reagent, control membrane protein, and an instruction manual. Corning Gentest P450 High Throughput Inhibitor Screening Kits are designed to rapidly screen for potential inhibitors of the principal drug metabolizing cytochrome P450 enzymes, CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. The IC50 or percent inhibition at a given substrate concentration, can be calculated and becomes the basis for comparison between a series of tested compounds. Details about this methodology can be found at www.corning.com/lifesciences. Log [I] Inhibition data collected using selective human P450 inhibitors and Corning Gentest fluorescent P450 assay technology. Corning Gentest Human Recombinant MDR1 Enzyme Screen for Human MDR1 (P-gp) Interactions w Faster, cheaper, and easier than cell-based assays w Simple HTS assay protocol w Established and validated technology Human P-gp (MDR1) is an ATP-dependent efflux pump capable of transporting many xenobiotics across cell membranes. High level expression of this protein has been linked to tumor resistance in chemotherapy. Chemicals that interact with MDR1 can be detected by measuring the increase in ATPase activity in membranes containing recombinant MDR1 versus membranes containing no recombinant enzyme (negative control). A method to perform a simple colorimetric ATPase assay in a 96 well plate is provided on the product insert. Greater methodological detail (including materials/reagents, preparation and storage of solutions, calculation of data, FAQs, references, and posters) is available at www.corning.com/lifesciences. The recombinant enzyme and ATPase assay method produces data that correlates well with data from cell-based transport assays.

Corning® Gentest™ Liver Tissue Fractions Screen for Metabolic Stability w Large variety of products w Multiple species w Minimal lot-to-lot variability Liver tissue fractions offer convenient and enriched sources of native enzymes for metabolic stability screening assays and other applications. The use of liver microsomes or S9 from various species to generate metabolite profiles helps to rapidly select an appropriate preclinical species to be used for future toxicity and pharmacokinetic studies. Our pooled liver fractions are formulated to represent an average profile of catalytic...

Animal Liver Microsomes 452401 Pooled Female Monkey (Cynomolgus) Pooled Female Monkey S9 (Cynomolgus) US sale only Pooled Male Rat (Sprague-Dawley) Pooled Female Rat (Sprague-Dawley) Pooled Male Rat (Wistar Han) Pooled Male Rat S9 (Sprague-Dawley) Pooled Male Dog (Beagle) Pooled Female Dog (Beagle) Pooled Male Dog S9 (Beagle) Pooled Male Mouse (CD-1) Pooled Female Mouse (CD-1) Pooled Male Mouse S9 (CD-1) Pooled Female Mouse S9 (CD-1) Pooled Male Mini-Pig (Gottingen) Pooled Male Mouse (B6C3F1) Pooled Female Guinea Pig (Dunkin Hartley) Pooled Male Guinea Pig (Dunkin Hartley) Pooled Male...

Corning acquired the Gentest™and Supersomes™ brands. For a listing of trademarks, visit us at www.corning.com/lifesciences/trademarks.