Bioactivity | Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research[1]. |
Target | IC50: 2.90 µM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa) |
Invitro | Edoxaban monohydrate (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner[1].Edoxaban monohydrate inhibits thrombin-induced platelet aggregation, with an IC50 of 2.90 µM[1]. Cell Viability Assay[1] Cell Line: |
In Vivo | Edoxaban monohydrate (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT[1]. Animal Model: |
Name | Edoxaban tosylate monohydrate |
CAS | 1229194-11-9 |
Formula | C31H40ClN7O8S2 |
Molar Mass | 738.27 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9. |