Characterization of anticoagulant properties of compoundC11-10 (7687521) in human plasma and full blood. (A) Prolongation of clotting time in platelet-poor human pooled plasma by C11-10. APTT was performed as described in the “Materials and methods” section, with varying amounts of C11-10 present (from 0-500 µM). A value for the prolongation of the APTT at 500 µM could not be obtained because this time exceeds 999 seconds and is thus not indicated in this graph. Data points are averages ± standard deviation from 3 measurements. (B) Influence of compound C11-10 in thrombin formation in PPP. Thrombin generation was triggered by 1 nM of FIXa in PPP in the presence of 4 µM of phospholipid vesicles (20% DOPS, 60% DOPC, 20% DOPE, mol/mol/mol), 30 µg/mL of CTI, and varying concentrations of compound C11-10 from 0 to 500 µM. Various concentrations of C11-10 are indicated by symbols: ● (0 µM), ▲ (100 µM), ▪ (200 µM), ○ (300 µM), △ (400 µM), and □ (500 µM). At 400 and 500 µM of C11-10 no thrombin was formed during the time of the experiment. (C) Inhibition of thrombin formation in PPP and PRP by compound C11-10. CAT was performed as described in the “Materials and methods” section, using PPP (○) or PRP (●). The thrombin peaks (in nM) are shown as a function of the final concentration of C11-10 present. Averages ± standard deviation are indicated, n = 3. (D) Influence on hemostasis in full blood by C11-10 as determined by ROTEM. ROTEM analysis was performed in full blood of a normal healthy individual in the absence (black graph) and presence (gray graph) of 500 µM of C11-10 after intrinsic trigger (1 mg/mL of kaolin) and a final concentration of 11.8 mM of CaCl₂ added.