Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 10,500 | |||
10 mg | 在庫あり | ¥ 14,500 | |||
25 mg | 在庫あり | ¥ 21,500 | |||
50 mg | 在庫あり | ¥ 27,000 | |||
100 mg | 在庫あり | ¥ 38,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,500 |
説明 | 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. |
別名 | Lixiana |
分子量 | 548.06 |
分子式 | C24H30ClN7O4S |
CAS No. | 480449-70-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 1mg/ml, Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Edoxaban 480449-70-5 Metabolism Proteases/Proteasome Factor Xa Thrombin Lixiana Inhibitor inhibitor inhibit