Edoxaban tosylate
Based on 9 publication(s) in Google Scholar
Edoxaban (DU-176b) tosylate 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 tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 480449-71-6
- 分子式: C31H38ClN7O7S2
- 分子量:720.26
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 Edoxaban tosylate
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]
生物活性
製品説明
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]
体外実験
Edoxaban tosylate (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner[1].
Edoxaban tosylate 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.
体内実験
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.
化学情報
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CAS 番号 480449-71-6
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性状 Solid
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分子量 720.26
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分子式 C31H38ClN7O7S2
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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.O=S(C5=CC=C(C)C=C5)(O)=O
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別名
DU-176b
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (69.42 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, 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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 2.5 mg/mL (3.47 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.
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
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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (392 KB)
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- Français - FR (392 KB)
- Deutsch - DE (392 KB)
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- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3884 mL | 6.9419 mL | 13.8839 mL | 34.7097 mL |
| 5 mM | 0.2777 mL | 1.3884 mL | 2.7768 mL | 6.9419 mL | |
| 10 mM | 0.1388 mL | 0.6942 mL | 1.3884 mL | 3.4710 mL | |
| 15 mM | 0.0926 mL | 0.4628 mL | 0.9256 mL | 2.3140 mL | |
| 20 mM | 0.0694 mL | 0.3471 mL | 0.6942 mL | 1.7355 mL | |
| 25 mM | 0.0555 mL | 0.2777 mL | 0.5554 mL | 1.3884 mL | |
| 30 mM | 0.0463 mL | 0.2314 mL | 0.4628 mL | 1.1570 mL | |
| 40 mM | 0.0347 mL | 0.1735 mL | 0.3471 mL | 0.8677 mL | |
| 50 mM | 0.0278 mL | 0.1388 mL | 0.2777 mL | 0.6942 mL | |
| 60 mM | 0.0231 mL | 0.1157 mL | 0.2314 mL | 0.5785 mL |