PK Induction in Heps
Assessment of a test compound's potential to induce the expression and activity of CYP1A2 and CYP3A4 enzymes.
Needs steward attention
Assay metadata
Rendered from the governed metadata model.
- Assay type hierarchy
- bioassay
- ›pharmacokinetic assay
- ›drug–drug interaction assay
- ›CYP induction assay
- ›hepatocyte induction assay
- Assay type *
- hepatocyte induction assay
- Experimental setting *
- in vitro
- Assay format *
- cell-based
- Assay design
- dose-response
- Target *
- CYP1A2CYP3A4
- Biological process
- enzyme induction
- Molecule role *
- inducer
- Cell system
- human hepatocytes
- Species
- Not set
- Donor source
- Not set
- Plating format
- Not set
- Incubation duration
- Not set
- Detection type *
- qPCRUPLC-MS/MS
- Physical detection method *
- PCR amplificationmass spectrometry
- Reference gene
- Not set
- Expected readout *
- fold inductionEmaxNOEL
Description
Assay to identify Induction of Human Cytochrome P450 Enzymes CYP1A2 and CYP3A4 in Long-Term Cultured Human Hepatocytes: Hepatocytes will be treated with multiple concentrations of test compounds (usually 14 - 30,000 ng/mL), along with positive controls omeprazole (CYP1A2 inducer) and rifampicin (CYP3A4 inducer), as well as vehicle control. Culture media will be prepared and changed daily over a 4 to 5-day treatment period. CYP induction will be assessed via quantitative PCR (qPCR) for mRNA levels. Specific enzyme activities will be measured by incubating hepatocytes with probe substrates for CYP1A2 and for CYP3A4, followed by LC/MS/MS analysis. The results will include an evaluation of whether the test compound acts as an inducer of mRNA and activity levels, indications of cell viability loss, signs of downregulation, as well as the concentrations of the No Observed Effect Level (NOEL) and the percentage of Emax values from the positive control.
Review history
This template has not been reviewed yet.
Change history
Imported from PK Induction in Heps.json
Dr Amelia Ostrowski · 18/08/2026, 19:33:36