Homepage
     
SERVICES in ADME-Tox
  ADME  
  Toxicology  
  V79 Cell Battery™  
  Analytical Services  
  Service Packages  
  Partnered Services  
 

GenPharmTox BioTech AG
phone: +49 (0) 89 89 55 59 - 0
eMail: info@genpharmtox.de
 
About us References Career News Publications Links Contact
Home   Imprint

CYP Inhibition

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

Drug Discovery Screen

The percentage inhibition of different CYP marker reaction activites by the test item is determined.


Quantity of test item required: 1 mg (pre-weighted)
Turnaround time of draft report: 15 working days


Study Design

  • multiple CYP isoforms (mircosomes or human recombinant enzymes)
  • triplicates
  • one concentration of CYP
  • 50 µM of test item
  • 30 min
  • neagtive controls: CYP marker reactions:
    1A1/2 (7-ethoxyresorufin O-deethylation)
    2A6 (coumarin 7-hydroxylation)
    2B6 (S-mephenyoin N-demethylation)
    2C8 (paclitaxel 6-hydroxylation)
    2C9 (diclofenac 4'-hydroxylation)
    2C19 (S-mephenytoin 4'-hydroxylation)
    2D6 (bufuralol hydroxylation)
    2E1 (chloroxazone 6a-hydroxylation)
    3A4/5 (testosterone 6b-hydroxylation)
    4A11 (lauric acid-hydroxylation)
    11B1 (11-deoxycortisol 11b-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 in the marker reaction

Please inquire for further phase I and II enzyme marker reactions and reference inhibitors
« back
GenPharmTox BioTech AG • phone: +49 (0) 89 89 55 59-0 • fax: +49 (0) 89 89 55 59-18 • eMail: info@genpharmtox.de

PDF Download
CYP Inhibition
[size 47 KB]
   
ADME
[size 129 KB]
Catalogue Services in ADME-Tox
[size 323 KB]