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Speed your selection of novel lead compounds

Vivid® CYP450 Screening Kits rapidly screen compounds early in the drug discovery process for Cytochrome P450-drug interactions and to generate data for predictive structure-activity relationship (SAR) modeling.  Vivid® CYP450 Screening Kits provide the high performance, throughput and reliability you need to speed selection of novel compounds for drug development.


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The Vivid® P450 Metabolism assays are:

  • Easy and homogenous – three step mix-and-read format, stop reagents optional
  • Rapid and flexible – kinetic or end point mode, at room temperature or 37ºC
  • Robust – high signal-to-background ratios and excellent Z’- factors
  • Able to be miniaturized – assays can be run in 96-, 384-, or 1536-well plates

Vivid® Substrates are blocked dyes that yield minimal fluorescence until oxidative cleavage occurs (Figure 1A). Metabolism at either of two potential cleavage sites releases the highly fluorescent product. P450 inhibitors are identified by their ability to prevent the production of the fluorescent metabolite. The three-step Vivid® screening assay (Figure 1B) is a simple mix-and-read protocol that does not require stop reagents to conduct the reaction in kinetic mode.

Vivid Screening Assay

Figure 1. The Vivid® screening assay.  A.  The Vivid® Substrate fluoresces when it is oxidized via P450 enzyme activity.  B.  A simple three step protocol is used to test compounds for their ability to inhibit P450 activity.  The test compound is added to a reaction containing P450 and the Vivid® Substrate, and the resulting fluorescence reflects the degree of inhibition of P450 activity.

 

Vivid® Kits and Substrates are available for a variety of P450 isozymes (Table 1). Each kit includes the isozyme-specific P450 BACULOSOMES® Plus Reagent, a Vivid® Substrate, and an NADPH regeneration system. The excitation and emission wavelengths of cleaved Vivid® Substrates are in the visible region and are subject to little or no fluorescent interference from NADPH or most test compounds.

 

Table 1. Choose the right Vivid® substrate for your needs. Structures of Vivid® substrates and standards.


Vivid Kits Substrates 

P450 activity can be inhibited by solvents commonly used to dissolve test compounds. The following sample data (Table 2) is intended as a guide for the selection and use of organic solvents. We always recommend including a solvent control in your experimental design.

 

Table 2. Values are given as percent inhibition at the indicated solvent concentration. Values preceded by a “+” indicate an increase in activity. Dashed lines indicate inhibition not detected.


Vivid Kits Substrates 

Ordering Information

Sku Name Size Price Qty
P2863 Vivid® CYP1A2 Blue Screening Kit 300 assays USD 347.68
P2856 Vivid® CYP3A4 Red Screening Kit 300 assays USD 347.68
P2857 Vivid® CYP3A4 Green Screening Kit 300 assays USD 347.68
P2858 Vivid® CYP3A4 Blue Screening Kit 300 assays USD 347.68
P2969 Vivid® CYP3A5 Green Screening Kit 300 assays USD 347.68
P2970 Vivid® CYP3A5 Blue Screening Kit 300 assays USD 347.68
P2859 Vivid® CYP2C9 Red Screening Kit 300 assays USD 347.68
P2860 Vivid® CYP2C9 Green Screening Kit 300 assays USD 347.68
P2861 Vivid® CYP2C9 Blue Screening Kit 300 assays USD 347.68
P2864 Vivid® CYP2C19 Blue Screening Kit 300 assays USD 347.68
P2972 Vivid® CYP2D6 Blue Screening Kit 300 assays USD 347.68
P2862 Vivid® CYP2D6 Cyan Screening Kit 300 assays USD 347.68
P3021 Vivid® CYP2E1 Blue Screening Kit 300 assays USD 347.68
P3019 Vivid® CYP2B6 Blue Screening Kit 300 assays USD 308.94
PV6140 Vivid® CYP2A6 Blue Screening Kit 300 assays USD 308.94
PV6141 Vivid® CYP2C8 Green Screening Kit 300 assays USD 308.94
PV6142 Vivid® CYP2J2 Cyan Screening Kit 300 assays USD 308.94