Table 1.
Inhibition of platelet aggregation and binding to PAR-1
| RWJ | Platelet aggregation IC50, μM
|
Binding IC50, μM | |||
|---|---|---|---|---|---|
| Thrombin | SFLLRN-NH2 | Collagen | U46619 | ||
| 53052 | 2.32 ± 0.11 (184) | 0.27 ± 0.01 (172) | IA | IA | 2.2 ± 0.5 (23) |
| 54399 | 0.57 ± 0.21 (8) | 0.18 ± 0.21 (10) | IA | IA | 0.82 ± 0.34 (4) |
| 56110 | 0.34 ± 0.04 (13) | 0.16 ± 0.06 (15) | IA | IA | 0.44 ± 0.21 (6) |
| 57269 | 0.22 ± 0.08 (4) | 0.08 ± 0.03 (3) | 4.7 ± 1.5 (2) | 24 ± 14 (2) | 0.025 ± 0.005 (2) |
Concentrations of agonists for aggregation studies: α-thrombin, 0.15 nM; SFLLRN-NH2, 2 μM; collagen, 3 μg/ml; U46619, 0.3 μM. Results are expressed as means ± SEM with number of experiments (N) in parentheses. IA denotes inactivity at 50 μM of test compound.