From: Cathepsin K inhibitors increase distal femoral bone mineral density in rapidly growing rabbits
Compound | Dose (mg/kg) | AUC (μm*hr) | Cmax(nM) | Cmin(nM) | Cl (mL/min/kg) | [Cmin]/bone res IC50 | IC50(nM) | |
---|---|---|---|---|---|---|---|---|
 |  |  |  |  |  |  | Rabbit CatK | Rabbit bone resorption assay |
L-833905 | 10 | 1.9 | 163 | 29 | – | 0.2 | 33 ± 2 | 149 ± 20 |
 | 30 | 6.1 | 651 | 60 | 0.4 |  |  | |
L-006235 | 1 | 0.3 | 74 | 9 | 113 | 1.8 | 0.5 | 5 ± 1 |
 | 3 | 1.0 | 337 | 15 | 3.0 |  |  | |
 | 10 | 5.0 | 2436 | 8 | 1.6 |  |  | |
L-873724 | 1 | 0.5 | 78 | <LOD* | 26 | ≤0.1 | 0.8 | 13 ± 1 |
 | 3 | 3.1 | 490 | 28 | 2.2 |  |  | |
 | 10 | 7.8 | 1370 | 32 | 2.5 |  |  | |
ODN | 0.3 | 0.7 | 33 | 35 | 6 | 1.5 | 1.0 | 23 ± 6 |
 | 1 | 2.2 | 130 | 37 | 1.6 |  |  | |
 | 3 | 4.1 | 270 | 88 |  | 3.8 |  |  |