AZ12971554 is a potent inhibitor of human thrombin with Ki = 0.3nM and activated partial thromboplastin time (APTT) IC50 = 0.68µM and Ecarin clotting time (ECT) IC50 = 0.16µM in human plasma. AZ12971554 demonstrates good selectivity towards other serine proteases with Trypsin I = 400, Trypsin IV = 100, FVIIa = 12750, FIXa = 4250, FXa = 675, FXIa = 1150, Kallekrein = 4700, t-PA = 775, Plasmin = 3450 and APC >11000 times selectivity. A prodrug of AZ12971554 has been administered orally to man in a limited Phase 1 study resulting in good bioavailability of the active compound.
MedKoo Cat#: 531501
Name: AZ12971554
CAS#: Unknown
Chemical Formula: C20H17ClFN7O3
Exact Mass: 457.1065
Molecular Weight: 457.85
Elemental Analysis: C, 52.47; H, 3.74; Cl, 7.74; F, 4.15; N, 21.42; O, 10.48
The following data is based on the product molecular weight 457.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
