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P450-Glo™ CYP2D6 Assay and Screening Systems

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A Luminescent Method and Screening System for Measuring CYP2D6 Activity

  • Screening system includes complete set of reagents
  • Luminescent format eliminates need for time-consuming analyses
  • Broad dynamic range and low background

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Catalog number selected: V8891

$ 154.00
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P450-Glo™ CYP2D6 Assay and Screening Systems
Assay System/10ml
$ 154.00
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The P450-Glo™ CYP2D6 Assay provides a homogeneous, luminescent method for measuring cytochrome P450 CYP2D6 activity. The assay employs luminogenic P450 substrates that are derivatives of beetle luciferin, a substrate for luciferase enzymes. The derivatives are not substrates for luciferase but are converted by P450s to luciferin, which in turn reacts with luciferase to produce light that is directly proportional to the activity of the P450.

This luminescent assay exhibits exquisite sensitivity, low background signals and broad dynamic range. It generates a "glow-type" luminescent signal, produced using derivatized luciferins as P450 substrates and a recombinant stabilized luciferase (Ultra-Glo™ Luciferase) coupled with a proprietary buffer system. The half-life of the luminescent output is greater than two hours, eliminating the need for luminometers with injectors and allowing batch plate processing. The luminescent format also eliminates the need for time-consuming analyses such as HPLC.

The luciferin-based substrates are readily taken up by cells and rapidly converted into luciferin inside the cell, which reduces the incubation time required (typically 30–60 minutes). Other benefits of the P450-Glo™ CYP2D6 Assay include a formulation that minimizes the incidence of false positives due to inhibition of luciferase by analytes when screening for cytochrome P450 inhibitors. Z´ values greater than 0.8 are achieved in either 96- or 384-well plate formats and confer highly predictive results.

The P450-Glo™ CYP2D6 Screening System provides a complete set of reagents for performing luminescent cytochrome P450 assays. The system include a membrane preparation containing recombinant human cytochrome P450 enzyme, a luminogenic cytochrome P450 substrate appropriate for the enzyme, an NADPH Regeneration System, reaction buffer, Luciferin Detection Reagent and Luciferin-Free Water. The membranes are prepared from baculovirus-infected insect cells and contain human cytochrome P450, P450 reductase, and cytochrome b5. The P450-Glo™ Screening System also contains a membrane fraction devoid of cytochrome P450 activity as a negative control. The assays are ideal for testing the effects of drugs and new chemical entities on cytochrome P450 enzyme activities.

Specifications

You are viewing: V8891 Change Configuration

What's in the box?

Item Part # Size

Reconstitution Buffer with Esterase

V144A 1 × 10ml

Luciferin Detection Reagent

V859A 1 × 1 each

Luciferin-ME EGE

V869A 1 × 240μg

SDS

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Download SDSPDF (232 KB) – English (United States)

Certificate of Analysis

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Use Restrictions

For Research Use Only. Not for Use in Diagnostic Procedures.

Storage Conditions

BB

 

Patents and Disclaimers

European Pat. No. 1131441 and Japanese Pat. No. 4520084.

U.S. Pat. Nos. 7,692,022 and 8,106,052 and other patents pending.

U.S. Pat. No. 8,288,559 and other patents pending.

U.S. Pat. No. 8,592,172 and other patents pending.

U.S. Pat. No. 8,551,721 and other patents pending.

Specifications

You are viewing: V8892 Change Configuration

What's in the box?

Item Part # Size

Reconstitution Buffer with Esterase

V144B 1 × 50ml

Luciferin Detection Reagent

V859B 1 × 1 each

Luciferin-ME EGE

V869B 1 × 900μg

SDS

Choose language:

Download SDSPDF (232 KB) – English (United States)

Certificate of Analysis

Search by lot number

Use Restrictions

For Research Use Only. Not for Use in Diagnostic Procedures.

Storage Conditions

BB

 

Patents and Disclaimers

European Pat. No. 1131441 and Japanese Pat. No. 4520084.

U.S. Pat. Nos. 7,692,022 and 8,106,052 and other patents pending.

U.S. Pat. No. 8,288,559 and other patents pending.

U.S. Pat. No. 8,592,172 and other patents pending.

U.S. Pat. No. 8,551,721 and other patents pending.

Specifications

You are viewing: V9890 Change Configuration

What's in the box?

Item Part # SizeConcentration

Reconstitution Buffer with Esterase

V144B 1 × 50ml

Luciferin-Free Water

V348A 1 × 50ml

Potassium Phosphate Buffer, 1M

V446A 1 × 5ml

Control Membranes

V476A 1 × 100μl5mg/ml

CYP2D6 (1pmol/μl) + Reductase

V489A 1 × 250μl

Luciferin Detection Reagent

V859B 1 × 1 each

Luciferin-ME EGE

V869B 1 × 900μg

Solution A—NADPH Regeneration System

V952A 1 × 2.75ml

Solution B—NADPH Regeneration System

V953A 1 × 600μl

SDS

Choose language:

Download SDSPDF (199 KB) – English (United States)

Certificate of Analysis

Search by lot number

Use Restrictions

For Research Use Only. Not for Use in Diagnostic Procedures.

Storage Conditions

 

Patents and Disclaimers

European Pat. No. 1131441 and Japanese Pat. No. 4520084.

U.S. Pat. Nos. 7,692,022 and 8,106,052 and other patents pending.

U.S. Pat. No. 8,288,559 and other patents pending.

U.S. Pat. No. 8,592,172 and other patents pending.

U.S. Pat. No. 8,551,721 and other patents pending.

Resources

Citations

  • Evaluation of Luminogenic Substrates as Probe Substrates for Bacterial Cytochrome P450 Enzymes: Application to Mycobacterium tuberculosis.


    --
    2019 SLAS Discov
  • See all citations

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