Overview

  • Product name

    CYP2D6 Activity Assay Kit (Fluorometric)
    See all CYP2D6 kits
  • Detection method

    Fluorescent
  • Sample type

    Cell Lysate, Microsomes, Tissue Lysate
  • Assay type

    Enzyme activity (quantitative)
  • Species reactivity

    Reacts with: Other species, Mammals
  • Product overview

    CYP2D6 Activity Assay Kit (Fluorometric) (ab211078) allows rapid measurement of native or recombinant cytochrome P450 2D6 (CYP2D6) activity in biological samples such as liver microsomes. The assay utilizes a non-fluorescent CYP2D6-selective substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 390/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. CYP2D6 specific activity is calculated by running parallel reactions in the presence and absence of the potent CYP2D6-selective inhibitor quinidine and subtracting any residual activity detected with the inhibitor present.


    The kit contains enough reagents to perform 100 sets of paired reactuibs (in presence/absence of inhibitor).

  • Notes

    Cytochrome P450 2D6 (CYP2D6, EC 1.14.14.1) is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolism enzymes. CYPs are membrane-bound hemeproteins responsible for Phase I biotransformation reactions, in which lipophilic drugs and other xenobiotic compounds are converted to more hydrophilic products to facilitate excretion from the body. CYP2D6 catalyzes oxidation of lipophilic bases with an aromatic ring and a nitrogen atom and is highly expressed in liver and brain tissue. The enzyme is responsible for metabolism of nearly 25% of all small molecule drugs commonly used by humans, particularly psychiatric drugs such as antidepressants, antipsychotics and stimulants. The CYP2D6 gene is highly polymorphic in the human population, with CYP2D6 activity ranging from complete metabolic deficiency to ultra-rapid metabolism. Due to this wide phenotypic variability, CYP2D6 is frequently implicated in drug toxicity and clinical drug/drug interactions.

  • Platform

    Microplate reader

Properties

Images

  • Typical AHMC standard calibration curve. One mol of AHMC corresponds to the metabolism of one mol of CYP2D6 substrate.

  • Reaction kinetics of fluorogenic substrate metabolism in human liver microsomes (0.5 mg/mL) at 37°C in the presence and absence of the selective CYP2D6 inhibitor quinidine (the no inhibitor reaction contained a final concentration of 0.5% acetonitrile).

  • Specific activity of CYP2D6 in pooled human liver microsome sample (0.5 mg/mL).

Protocols

References

ab211078 has not yet been referenced specifically in any publications.

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