Plasma protein binding of 14C-DB289 and 14C-DB75 in vitro
Results represent the mean of duplicate determinations.
Species/Analyte | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Plasma Concentrationa | Mouse | Rat | Rabbit | Monkey | Human | ||||||||||||||
| DB289 | DB75 | DB289 | DB75 | DB289 | DB75 | DB289 | DB75 | DB289 | DB75 | ||||||||||
| 2 ng/ml | - | 78.5 | - | 81.3 | - | - | - | - | - | - | |||||||||
| 3 ng/ml | - | - | - | - | - | 94.5 | - | - | - | - | |||||||||
| 5 ng/ml | - | - | - | - | - | - | - | - | - | 77.1 | |||||||||
| 10 ng/ml | - | 78.0 | - | 78.9 | - | 91.6 | - | - | - | 77.2 | |||||||||
| 20 ng/ml | - | 81.6 | - | 82.2 | - | - | - | 96.7 | - | 76.1 | |||||||||
| 30 ng/ml | - | - | - | - | 97.6 | 86.4 | - | - | - | - | |||||||||
| 50 ng/ml | 98.6 | 81.7 | 98.8 | 81.0 | - | - | 98.7 | 93.7 | 98.6 | 77.5 | |||||||||
| 100 ng/ml | - | 84.1 | - | 80.4 | 97.6 | - | 98.2 | 89.1 | 98.5 | 75.2 | |||||||||
| 200 ng/ml | 98.4 | 83.7 | 98.6 | 81.3 | - | - | - | - | 98.2 | - | |||||||||
| 250 ng/ml | - | - | - | - | - | - | 97.7 | - | - | - | |||||||||
| 300 ng/ml | - | - | - | - | 97.6 | - | - | - | - | - | |||||||||
| 500 ng/ml | 98.5 | - | 98.7 | - | - | - | - | - | - | - | |||||||||
| 1000 ng/ml | 98.3 | - | 98.7 | - | 97.3 | - | - | - | - | - | |||||||||
-. not measured.
↵ a Concentrations are nominal values and are expressed in terms of DB289 and DB75 free base.