CYP Inhibition Express
XenoTech's CYP Inhibition Express is more than just a screening service. Our 96-well plate format combines both direct and time-dependent inhibition information and offers a variety of compound and CYP enzyme combinations to provide accurate and reliable data. CYP Inhibition Express is a non-GLP service that provides our customers with a data summary of results in about a week.
STUDY DETAILS
ASSAY SELECTION
XenoTech offers the flexibility for our customers to combine assays and compounds on a single inhibition express plate. Each plate can consist of 12 enzymatic assays/1 compound, 1 enzymatic assay/12 compounds, or any other combination of 12 samples per plate as desired.
We recommend the following assays:
CYP1A2 Phenacetin O-deethylation
CYP2B6 Efavirenz 8-hydroxylation
CYP2C8 Amodiaquine N-dealkylation
CYP2C9 Diclofenac 4´-hydroxylation
CYP2C19 S-Mephenytoin 4´-hydroxylation
CYP2D6 Dextromethorphan O-demethylation
CYP3A4/5 Midazolam 1´-hydroxylation
CYP3A4/5 Testosterone 6β-hydroxylation
Additional validated assays available:
CYP2A6 Coumarin 7-hydroxylation
CYP2B6 Bupropion hydroxylation
CYP2C8 Paclitaxel 6α-hydroxylation
CYP2D6 Bufuralol 1´-hydroxylation
CYP2E1 Chlorzoxazone 6-hydroxylation
CYP3A4/5 Nifedipine oxidation
CYP3A4/5 Atorvastatin o-hydroxylation
CYP4A11 Lauric acid 12-hdyroxylation
TEST SYSTEM Pool of 16 individuals, mixed gender, human liver microsomes
INCUBATION CONDITIONS Protein concentration: less than 0.1 mg/mL
Incubation time: 5 minutes
Time-dependent pre-incubation: 30 minutes
AUTOMATION AND ANALYSIS Tecan liquid-handling system
Validated LC/MS/MS methods
High-throughput Shimadzu autosamplers
Deuterated internal standards
RESULTS Direct inhibition measured over four concentrations
Time-dependent inhibition measured over two concentrations
Data summary in about a week
OPTIONAL SERVICES IC50 estimates (if the data allow)
Assessment of solubility
Consultation on results
RELATED INFORMATION
FDA’S latest guidance document (PDF)
XenoTech Products: Human Liver Microsomes