1. Metabolic Enzyme/Protease
  2. Factor Xa
    Thrombin
  3. Edoxaban

Edoxaban (Synonyms: DU-176)

Cat. No.: HY-10264 Purity: 99.03%
Handling Instructions

Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.

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Edoxaban Chemical Structure

Edoxaban Chemical Structure

CAS No. : 480449-70-5

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Description

Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].

IC50 & Target

Ki: 0.561 nM (Free FXa); 2.98 nM (Prothrombinase); 6.00 μM (Thrombin) and 41.7 μM (Factor IXaβ)[1]

In Vitro

Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with Ki 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 manner, 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) (IC50: 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) dose-dependently inhibits thrombus formation in rat thrombosis models[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.
Clinical Trial
Molecular Weight

548.06

Formula

C₂₄H₃₀ClN₇O₄S

CAS No.

480449-70-5

SMILES

O=C(N(C)C)[[email protected]@H](CC1)C[[email protected]]([[email protected]]1NC(C(NC(C=C2)=NC=C2Cl)=O)=O)NC(C3=NC(CC4)=C(CN4C)S3)=O

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (18.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8246 mL 9.1231 mL 18.2462 mL
5 mM 0.3649 mL 1.8246 mL 3.6492 mL
10 mM 0.1825 mL 0.9123 mL 1.8246 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

EdoxabanDU-176DU176DU 176Factor XaThrombinFxaFXaanticoagulantatrialfibrillationCYP3A4strokeantithromboticFIXathromboembolicInhibitorinhibitorinhibit

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