CYP Induction in Cryopreserved Human Hepatocytes
- Plated cryopreserved human hepatocytes from 3 individual donors
- Induction of CYP1A2, CYP2B6 and CYP3A4 by test compound measured by comparing enzyme activity of hepatocytes treated with test compound with vehicle control
- Optionally, test compound concentration can be monitored during treatment in accordance with 2017 FDA guidance “In Vitro Metabolism- and Transporter-Mediated Drug-Drug Interaction Studies”
|Test Compound Concentration||30 µM, 3 µM, and 0.3 µM|
|Percent Organic Solvent – Inducer Treatment||0.1% DMSO|
|Percent Organic Solvent – Substrate Incubation||1.5% acetonitrile|
|Inducer Treatment Time||48 hours|
|Substrate Incubation Time||30 minutes|
|Treatment and Incubation Conditions||37 °C, 5% CO2, and saturating humidity|
|Positive Control||Omeprazole (1A2), Phenobarbital (2B6), and Rifampicin (3A4)|
|Number of Repeats||3|
Deliverable: Mean fold induction of test compound and positive control compound.
Test Compound Requirement: 2-3 mg dry powder or 100-200 µL of 30 mM DMSO stock solution.