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GenPharmTox BioTech AG
phone: +49 (0) 89 89 55 59 - 0
eMail: info@genpharmtox.de
 
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CYP Inhibition

The inhibition of CYP isoenzymes is one of the key aspects in drug-drug interaction.

Determination of the Ki

The Ki of the test item for a specific CYP isoform marker reaction or drug-drug interaction is determined.


Quantity of test item required: 20 mg
Turnaround time of draft report: 20 working days


Study Design

  • one CYP isoform (microsomes or human recombinant enzymes)
  • triplicates
  • one concentration of CYP
  • three to six concentrations of marker substrate
  • three to six concentrations of test item
  • one time point
  • negative controls: CYP marker reactions:
    1A1/2 (7-ethoxyresorufin O-deethylation)
    2A6 (coumarin 7-hydroxylation)
    2B6 (S-mephenytoin N-demethylation)
    2C8 (paclitaxel 6a-hydroxylation)
    2C9 (diclofenac 4'-hydroxylation)
    2C19 (S-mephenytoin 4'-hydroxylation)
    2D6 (bufuralol-hydroxylation)
    2E1 (chloroxazone 6-hydroxylation)
    3A4/5 (testosterone 6ß-hydroxylation)
    4A11 (lauric acid-hydroxylation)
    11B1 (11-deoxycortisol 11ß-hydroxylation)
    11B2 (deoxycorticosterone-hydroxylation)
  • positive controls: CYP reference inhibitors
    1A1/2 (furafylline)
    2A6 (8-methoxypsoralene)
    2B6 (triethylenethiophosphoramide)
    2C8 (ketoconazole)
    2C9 (sulfaphenazole)
    2C19 (omeprazole)
    2D6 (quinidine)
    2E1 (diethyldithiocarbamate)
    3A4/5 (ketoconazole)
    4A11 (10-(imidazolyl)-decanoic acid)
    11B1 (metyrapone)
    11B2 (ketoconazole)


Analytics

  • detection of metabolite formed during marker reaction


Please inquire for further phase I and II enzyme marker reactions and refernce inhibitors.

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GenPharmTox BioTech AG • phone: +49 (0) 89 89 55 59-0 • fax: +49 (0) 89 89 55 59-18 • eMail: info@genpharmtox.de

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