June 25, 2018
Assay System:
- Cryopreserved mammalian hepatocytes in suspension.
- Human hepatocytes are pooled from 10 donors (mixed gender). All other species are male.
- Metabolic clearance determined by measuring percent remaining of test compound at multiple time points during incubation with hepatocytes.
Assay Conditions:
Test Compound Concentration | 1 µM |
Hepatocyte Concentration | 106 viable cells/mL |
Percent Organic Solvent in Incubation | 0.1% DMSO |
Incubation Time | 0, 15, 30, 60, 90, and 120 minutes |
pH | 7.4 |
Temperature | 37 °C |
Positive Control | Testosterone and 7-hydroxycoumarin |
Analysis | LC-MS |
Number of Repeats | 2 |
Deliverable: Intrinsic clearance, (µL/min/106 cells), t1/2, and predicted blood extraction ratio (EH).
Test Compound Requirement: 1-2 mg dry powder or 100-200 µL of 10 mM DMSO stock solution.