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Edoxaban

Catalog No. T2368L CAS 480449-70-5

Synonyms: Lixiana

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].

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Edoxaban, CAS 480449-70-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 63.00
25 mg	In stock	$ 93.00
50 mg	In stock	$ 118.00
100 mg	In stock	$ 164.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.6%

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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.

Synonyms	Lixiana
Molecular Weight	548.06
Formula	C24H30ClN7O4S
CAS No.	480449-70-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 130 mM

References and Literature

1. Furugohri T, et al. J Thromb Haemost. 2008, 6(9), 1542-1549.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Pediatric Drug Library Anti-Cardiovascular Disease Compound Library Orally Active Compound Library FDA-Approved & Pharmacopeia Drug Library Protease Inhibitor Library Bioactive Lipid Compound Library Drug-induced Liver Injury (DILI) Compound Library

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Keywords

Edoxaban 480449-70-5 Metabolism Proteases/Proteasome Factor Xa Thrombin Lixiana inhibitor inhibit

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