Overview

  • Product name

    CYP3A4 Activity Assay Kit (Fluorometric)
    See all CYP3A43 kits
  • Detection method

    Fluorescent
  • Sample type

    Cell Lysate, Microsomes, Tissue Lysate
  • Assay type

    Quantitative
  • Species reactivity

    Reacts with: Other species, Mammals
  • Product overview

    CYP3A4 Activity Assay Kit (Fluorometric) (ab211076) allows rapid measurement of native or recombinant CYP3A4 activity in biological samples such as liver microsomes. The assay utilizes a non-fluorescent CYP3A4 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 535/587 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. CYP3A4 specific activity is calculated by running parallel reactions in the presence and absence of the potent inhibitor Ketoconazole and subtracting any residual activity detected with the inhibitor present.


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

  • Notes

    Cytochrome P450 3A4 (CYP3A4, EC 1.14.13.157) 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 transformed to more hydrophilic products to facilitate excretion from the body. CYP3A4 is expressed in high levels in the liver and intestines, where it catalyzes oxidation of an extraordinarily wide variety of structurally distinct ligands. More than half of all small molecule drugs commonly used by humans are metabolized by CYP3A4. Inhibition of CYP3A4-mediated metabolism is a common cause of adverse drug/drug and drug/food interactions and toxicity. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form, CYP3A4 inhibition can lead to decreased drug efficacy.

  • Platform

    Microplate reader

Properties

Images

  • Typical Resorufin standard calibration curve. One mole of resorufin corresponds to the metabolism of one mole of CYP3A4 substrate.

  • Reaction kinetics of fluorogenic substrate metabolism in human liver microsomes (0.05 mg/mL) at 37°C in the presence and absence of the CYP3A4 inhibitor Ketoconazole ("no inhibitor" reaction contained a final concentration of 0.6% acetonitrile).

  • Specific activity of CYP3A4 in pooled human liver microsomes (0.05  mg/mL).

Protocols

References

ab211076 has not yet been referenced specifically in any publications.

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