Results of microsome stability studies (expressed as T1/2), protein binding experiments [expressed as fraction unbound (fu)], calculated hepatic clearance (Clhepatic), and compound extracted per pass for five Y2R antagonists and BIIE0246
| ID and Species | T1/2 | fu | Clhepatic | Extracted per Pass |
|---|---|---|---|---|
| min | % | |||
| SF-11 | ||||
| Mouse | 4 | 0.03 | 5.7 | 6.3 |
| Rat | 3 | 0.02 | 6.1 | 11 |
| Human | 10 | 0.01 | 0.3 | 1.4 |
| SF-21 | ||||
| Mouse | 1 | 0.82 | 90 | 100 |
| Rat | 1 | 0.13 | 50 | 90 |
| Human | 8 | 0.23 | 7 | 34 |
| SF-22 | ||||
| Mouse | 1 | 1 | 90 | 100 |
| Rat | 1 | 0.19 | 53 | 96 |
| Human | 6 | 0.28 | 10 | 49 |
| SF-31 | ||||
| Mouse | 14 | 0.12 | 6.4 | 7.2 |
| Rat | 6 | 0.07 | 10 | 18 |
| Human | 13 | 0.07 | 1.5 | 7.4 |
| SF-41 | ||||
| Mouse | 4 | 0.39 | 51 | 57 |
| Rat | 1 | 0.19 | 53 | 96 |
| Human | 3 | 0.19 | 12 | 60 |
| BIIE0246 | ||||
| Mouse | 166 | 0.079 | 0.4 | 0.4 |
| Rat | 27 | 0.022 | 0.8 | 1.4 |
| Human | 23 | 0.015 | 0.2 | 0.9 |