Metabolic Stability of Low Clearance Compounds
Sygnature’s routine hepatocyte stability assay monitors the disappearance of a substrate in suspension, over 1-2 hours incubation. Evaluating low clearance compounds can be a challenge using existing methods. To accurately determine intrinsic clearance and half-life values of low clearance compounds, Sygnature has developed a method utilising primary human hepatocytes in culture, enabling longer incubation times (typically 24 hours). Data output consists of mean intrinsic clearance (Clint) and half-life (t1/2) measurements.
|Compound requirements||10 mM in DMSO, 20µL|
|Test Article Concentration||1 µM|
|Hepatocyte Concentration||0.35 x 106 cells / well|
|Incubation Conditions||Up to 24 hours at 37°C|
|Time Points||0, 1, 2, 4, 18, 24 hours|
|Controls||2 Positive controls|
|Data Delivery||Clint (µL/min/1×106 cells), Half-life (min)|
Figure 1 Control compound CLint data for n=3 experiments.
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