R-1663 is a factor Xa inhibitor potentially for the treatment of thrombosis. R-1663 prolonged clotting times, inhibited thrombin generation (peak height and endogenous thrombin potential [ETP]) and anti-factor Xa activity in a concentration-dependent manner without increasing bleeding time. Pharmacodynamic parameters were strongly correlated to R-1663 plasma concentrations. The inhibition was more pronounced on peak height (IC₅₀ = 194 ng/ml) than on ETP (2790 ng/ml). Pharmacokinetics and pharmacodynamics of R-1663 appeared not to be substantially affected by age or gender but remained to be confirmed in larger clinical trials including older patients.
MedKoo Cat#: 528205
Name: R-1663
CAS#: 865451-66-7
Chemical Formula: C22H23ClN4O5
Exact Mass: 458.1357
Molecular Weight: 458.90
Elemental Analysis: C, 57.58; H, 5.05; Cl, 7.73; N, 12.21; O, 17.43
The following data is based on the product molecular weight 458.90 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 |
