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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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