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

Edoxaban tosylate monohydrate (Synonyms: DU-176b monohydrate)

Cat. No.: HY-10264B Purity: 99.85%
Handling Instructions

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

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Edoxaban tosylate monohydrate Chemical Structure

Edoxaban tosylate monohydrate Chemical Structure

CAS No. : 1229194-11-9

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Description

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

738.27

Formula

C₃₁H₄₀ClN₇O₈S₂

CAS No.

1229194-11-9

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.O=S(C5=CC=C(C)C=C5)(O)=O.O

Shipping

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 : 50 mg/mL (67.73 mM; Need ultrasonic)

H2O : 1 mg/mL (1.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3545 mL 6.7726 mL 13.5452 mL
5 mM 0.2709 mL 1.3545 mL 2.7090 mL
10 mM 0.1355 mL 0.6773 mL 1.3545 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 (3.39 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (3.39 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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Keywords:

Edoxaban tosylateDU-176bFactor XaThrombinFxaFXaanticoagulantatrialfibrillationCYP3A4strokeantithromboticFIXathromboembolicInhibitorinhibitorinhibit

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Edoxaban tosylate monohydrate
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