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Metabolic stability of KGW44 and KGW59.
| Compound ID | Microsome species | T1/2 (min) | CLint, in vitro (μL/min/mg protein) | Predicted EH |
|---|---|---|---|---|
| KG81 | Human | 9 | 129 | 0.88 |
| Mouse | <2 | >886 | N/A | |
| KGW44 | Human | 83 | 21 | 0.45 |
| Mouse | 9 | 99 | N/A | |
| KGW59 | Human | 111 | 16 | 0.38 |
| Mouse | 37 | 46 | 0.50 |
Metabolic stability was assessed in both human and mouse liver microsomes. The half-life (T1/2), intrinsic clearance in vitro (CLint), and the predicted hepatic extraction ratios (EH) were determined (Sanford et al., 20181).
