CYP (Cytochrome P450)

In drug discovery, the effects of compounds on the metabolic reactions specific for various human drug-metabolizing enzymes have been routinely examined. Cytochrome P450 inhibition assay screening test is useful in the investigation of clinical drug-drug interactions (DDI) studies for new drugs

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CYP Substrate

Testosterone

Testosterone, a well known steroid hormone, is used in Cytochrome P450 (CYP) metabolism inhibition and CYP induction drug interaction studies. The metabolism of testosterone to its hydroxy form, 6β-hydroxytestosterone (6β-OH-T) is a commonly used assay to evaluate human CYP3A enzyme activities.

Reaction in vivo

Conversion of testosterone to 6β-hydroxytestosterone reaction is used to determine enzyme activity of CYP3A4.

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Example

It is used as a substrate for pharmacokinetics experiments to add to a cell together with a candidate compound that can be a drug and confirm whether it affects drug metabolism.

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HPLC Charts

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    teststeron (commercial product)
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    6β-hydroxytestosterone
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    purified teststeron (code: 200-20761)
  • HPLC Conditions
    Column Wakopak® Wakosil®-Ⅱ 5C18HG, 4.6mmφ x 250mm
    Temp. 40℃
    Eluent A: water B: acetonitrile
    Flow 1.0 mL/min
    Detector UV 240 nm
  • Eluent Conditions
    Time (min.) A (%) B (%)
    1 - 10 50 50
    10 - 20 50 → 10 50 → 90
    20 - 30 10 90

Product List

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CYP Substrate

CYP Inhibitor

CYP Inducer

CYP Metabolite

CYP for Fluorescent Assay

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CYP Substrate

Author: A. Samoveanu

For research use or further manufacturing use only. Not for use in diagnostic procedures.

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