| Name | Edoxaban |
| Description | Edoxaban (Lixiana) (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3]. |
| In vitro | Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with K i values of 6.90 nM, 0.715 nM and 0.457 nM, respectively [1]. Prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT) of human plasma are prolonged by Edoxaban (DU-176b) in a concentration-dependent way, doubling PT and APTT at 0.256 and 0.508 μM, respectively. The double clotting time (CT2) for TT, however, was much higher (4.95 μM), reflecting its anti-thrombin activity. Thrombin-induced platelet aggregation is inhibited by a high concentration of Edoxaban (DU-176b) (IC 50 : 2.90 μM), reflecting its weak anti-thrombin activity [1]. Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein [2]. |
| In vivo | Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) inhibits thrombus formation in rat thrombosis models in a dose-dependent manner [1]. Animal Model: Wistar rats (210-240 g) with venous stasis thrombosis model [1] Dosage: 0.5 mg/kg, 2.5 mg/kg, 12.5 mg/kg Administration: Oral administration Result: Dose-dependently inhibited thrombus formation in rat thrombosis models. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mg/mL (18.25 mM), Sonication is recommended.
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| Keywords | Thrombin | FactorXa | Factor Xa | Edoxaban |
| Inhibitors Related | Dabigatran Etexilate Mesylate | (S)-(+)-Ibuprofen | AEBSF hydrochloride | Heparin sodium salt | Ozagrel | Dabigatran etexilate | Apixaban | 2-Methoxyphenothiazine | Rivaroxaban | Coumarin | p-Hydroxycinnamic acid | Fondaparinux sodium |
| Related Compound Libraries | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | NMPA-Approved Drug Library |
United States
