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

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

Cat. No.: HY-10264B Purity: 99.91%
SDS COA Handling Instructions

Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research.

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

Edoxaban tosylate monohydrate Chemical Structure

Edoxaban tosylate monohydrate Chemical Structure

CAS No. : 1229194-11-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 89 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 143 In-stock
100 mg USD 198 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Edoxaban tosylate monohydrate:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Kis of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research[1].

IC50 & Target

IC50: 2.90 µM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa)[1]

In Vitro

Edoxaban monohydrate (1, 1 and 5 minutes respectively) prolongs PT, TT and APTT of human plasma in a concentration-dependent manner[1].
? Edoxaban monohydrate inhibits thrombin-induced platelet aggregation, with an IC50 of 2.90 μM[1].

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

Cell Viability Assay[1]

Cell Line: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet
Concentration:
Incubation Time: 1 and 5 minutes
Result: Antithrombin.
In Vivo

Edoxaban monohydrate (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT[1].

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

Animal Model: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model)[1].
Dosage: 0.5, 2.5 and 12.5 mg/kg
Administration: Oral administration; once
Result: Inhibited exogenous FXa activity.
Antithrombotic.
Clinical Trial
Molecular Weight

738.27

Formula

C31H40ClN7O8S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C)C)[C@@H](CC1)C[C@H]([C@H]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

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 : 50 mg/mL (67.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.3545 mL 6.7726 mL 13.5452 mL 33.8629 mL
DMSO 5 mM 0.2709 mL 1.3545 mL 2.7090 mL 6.7726 mL
10 mM 0.1355 mL 0.6773 mL 1.3545 mL 3.3863 mL
15 mM 0.0903 mL 0.4515 mL 0.9030 mL 2.2575 mL
20 mM 0.0677 mL 0.3386 mL 0.6773 mL 1.6931 mL
25 mM 0.0542 mL 0.2709 mL 0.5418 mL 1.3545 mL
30 mM 0.0452 mL 0.2258 mL 0.4515 mL 1.1288 mL
40 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8466 mL
50 mM 0.0271 mL 0.1355 mL 0.2709 mL 0.6773 mL
60 mM 0.0226 mL 0.1129 mL 0.2258 mL 0.5644 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Edoxaban tosylate monohydrate
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