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

Edoxaban tosylate (Synonyms: DU-176b)

Cat. No.: HY-10264A Purity: 99.47%
Handling Instructions

Edoxaban tosylate (DU-176b) 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 tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate 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 tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.

For research use only. We do not sell to patients.

Edoxaban tosylate Chemical Structure

Edoxaban tosylate Chemical Structure

CAS No. : 480449-71-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 143 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 640 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Description

Edoxaban tosylate (DU-176b) 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 tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate 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 tosylate 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

720.26

Formula

C31H38ClN7O7S2

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (138.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3884 mL 6.9419 mL 13.8839 mL
5 mM 0.2777 mL 1.3884 mL 2.7768 mL
10 mM 0.1388 mL 0.6942 mL 1.3884 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Edoxaban tosylate
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HY-10264A
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