Edoxaban
Based on 9 publication(s) in Google Scholar
Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research.
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- Purity: 99.81%
- CAS No.: 480449-70-5
- 화학식: C24H30ClN7O4S
- 분자량:548.06
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Edoxaban
More- J Thromb Haemost. 2025 Jun;23(6):1938-1952. [Abstract]
- Molecules. 2023 Feb 28;28(5):2254. [Abstract]
- Thromb Res. 2021 Jan:197:141-143. [Abstract]
- PLoS One. 2024 May 15;19(5):e0292628. [Abstract]
- Virology. 2023 Aug:585:205-214. [Abstract]
- LabMed. 2024 Nov 18.
- SSRN. 2025 Dec 1.
- Authorea. 2023 Apr 17.
- Elife. 2022 Mar 23:11:e77444. [Abstract]
Biological Activity
제품 설명
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]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
2.9 μM
Compound: Edoxaban
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Inhibition of thrombin-induced human platelet aggregation preincubated for 2 to 4 mins followed by thrombin addition
Inhibition of thrombin-induced human platelet aggregation preincubated for 2 to 4 mins followed by thrombin addition
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[PMID: 36758304] |
| Platelet | IC50 |
2.9 μM
Compound: Savaysa
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Inhibition of alpha-thrombin induced human Platelet aggregation
Inhibition of alpha-thrombin induced human Platelet aggregation
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[PMID: 38889609] |
In Vitro
Edoxaban (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner[1].
Edoxaban 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.
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Cell Line:Human, rat, cynomolgus monkey and rabbit plasma; Human platelet
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Concentration:
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Incubation Time:1 and 5 minutes
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Result:Antithrombin.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:0.5, 2.5 and 12.5 mg/kg
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Administration:Oral administration; once
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Result:Inhibited exogenous FXa activity.
Antithrombotic.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 480449-70-5
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Appearance Solid
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분자량 548.06
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화학식 C24H30ClN7O4S
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Color White to off-white
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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
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Synonyms
DU-176
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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J Thromb Haemost
2025 Jun;23(6):1938-1952. PMID: 40122463 -
Molecules
Generic Methods for Simultaneous Analysis of Four Direct Oral Anticoagulants in Human Plasma and Urine by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry. [Abstract]2023 Feb 28;28(5):2254. PMID: 36903499 -
Thromb Res
Dielectric blood coagulometry as a means of evaluating the change in thrombin generation induced by direct oral anticoagulants. [Abstract]2021 Jan:197:141-143. PMID: 33217621 -
PLoS One
Xa inhibitor edoxaban ameliorates hepatic ischemia-reperfusion injury via PAR-2-ERK 1/2 pathway. [Abstract]2024 May 15;19(5):e0292628. PMID: 38748746 -
Virology
Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]2023 Aug:585:205-214. PMID: 37384967 -
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Elife
2022 Mar 23:11:e77444. PMID: 35294338
용액&용해도
In Vitro:
DMSO : 10 mg/mL (18.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.82 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8246 mL | 9.1231 mL | 18.2462 mL | 45.6154 mL |
| 5 mM | 0.3649 mL | 1.8246 mL | 3.6492 mL | 9.1231 mL | |
| 10 mM | 0.1825 mL | 0.9123 mL | 1.8246 mL | 4.5615 mL | |
| 15 mM | 0.1216 mL | 0.6082 mL | 1.2164 mL | 3.0410 mL |
Edoxaban Related Classifications
HY-10264 Related Classifications
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