Edoxaban tosylate (C09-1130-895)

Edoxaban (DU-176b) tosylate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K i s of 0.561 and 2.98 nM for free human FXa and prothrombinase . Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease researchIn VitroEdoxaban tosylate (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner. Edoxaban tosylate inhibits thrombin-induced platelet aggregation, with an IC 50 of 2.90 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet Concentration: Incubation Time: 1 and 5 minutes Result: Antithrombin.In VivoEdoxaban tosylate (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model) . Dosage: 0.5, 2.5 and 12.5 mg/kg Administration: Oral administration; once Result: Inhibited exogenous FXa activity. Antithrombotic.Form:SolidIC50& 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). Specification: 0.99 Molecular Formula: C31H38ClN7O7S2 Molecular Weight: 720.26 EC Number: 852-705-5 PubChem CID: 44610678 Isomeric SMILES: CC1=CC=C(C=C1)S(=O)(=O)O.CN1CCC2=C(C1)SC(=N2)C(=O)N[C@@H]3C[C@H](CC[C@@H]3NC(=O)C(=O)NC4=NC=C(C=C4)Cl)C(=O)N(C)C