Table 2. Effect of dabigatran, argatroban, or DAPA on thrombin binding to γA/γA-fibrin, γA/γ′-fibrin, factor Va, or GpIbα269-286ppp.
The effect of 0–5000 nM dabigatran, argatroban, or DAPA on the binding of thrombin to immobilized γA/γA-fibrin, γA/γ′-fibrin, factor Va or GpIbα269-286ppp was quantified using SPR. EC50 values were determined by plotting the Req values against the inhibitor concentration and fitting by nonlinear regression analysis using BIAevaluation software. Change is the calculated difference between thrombin binding in the absence of inhibitors and that determined at saturating inhibitor concentration. Values are shown as mean ± S.D. for three separate experiments.
| Dabigatran | Argatroban | DAPA | ||||
|---|---|---|---|---|---|---|
| Target | EC50 (nM) | Change (%) | EC50 (nM) | Change (%) | EC50 (nM) | Change (%) |
| γA/γA-fibrin | 184.6 ± 4.3 | - 47.6 ± 0.4 | 62.4 ± 4.8 | + 47.2 ± 1.0 | 514.1 ± 24.0 | + 25.1 ± 0.5 |
| γA/γ′-fibrin | 182.4 ± 15.0 | - 28.4 ± 1.6 | 59.4 ± 5.1 | + 44.5 ± 2.3 | 515.9 ± 31.0 | + 27.7 ± 1.5 |
| Factor Va | 204.2 ± 17.0 | - 37.9 ± 3.2 | 23.4 ± 8.8 | + 15.1 ± 3.9 | 565.1 ± 200 | + 13.2 ± 3.2 |
| GpIbα269-286ppp | — | 0 | 161.0 ± 2.6 | +17.3 ± 0.6 | 1288.3 ± 32.3 | +25.4 ± 0.0 |