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| 250mg |
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Edoxaban tosylate (DU176b; DU-176; trade name Savaysa; Lixiana), the tosylate salt of edoxaban, is a marketed anticoagulant drug acting as a potent, selective, orally bioavailable and direct factor Xa inhibitor. It inhibits Factor Xa with a Ki of 0.561 nM, and exhibits >10 000-fold selectivity over thrombin and FIXa. Edoxaban was developed by Daiichi Sankyo and was approved in July 2011 in Japan for prevention of venous thromboembolisms (VTE) following lower-limb orthopedic surgery. It was also approved by the FDA in January 2015 for the prevention of stroke and non–central-nervous-system systemic embolism.
| ln Vitro |
Human plasma PT, TT, and APTT are prolonged by edoxaban tosylate in a concentration-dependent manner (1, 1, and 5 minutes, respectively) [1]. With an IC50 of 2.90 µM, edoxaban tosylate suppresses platelet aggregation induced by thrombin[1].
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| ln Vivo |
Edoxaban tosylate (0.5, 2.5, and 12.5 mg/kg; oral; once) prolongs prothrombin time (PT) and decreases thrombosis in a significant and dose-dependent manner [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: human, rat, cynomolgus monkey, rabbit plasma; human platelet Tested Concentrations: Incubation Duration: 1 and 5 minutes Experimental Results: Antithrombin. |
| Animal Protocol |
Animal/Disease Models: Male Slc: Wistar rat (210-240g); male New Zealand white rabbit (2.5-3.5kg) (both are venous stasis and thrombosis models) [1].
Doses: 0.5, 2.5 and 12.5 mg/kg Route of Administration: Oral; Primary Experimental Results:Inhibition of exogenous FXa activity. Anti-thrombotic. |
| References |
[1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.
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| Molecular Formula |
C₃₁H₃₈CLN₇O₇S₂
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|---|---|
| Molecular Weight |
720.26
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| CAS # |
480449-71-6
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| Related CAS # |
Edoxaban;480449-70-5;Edoxaban tosylate monohydrate;1229194-11-9;Edoxaban hydrochloride;480448-29-1
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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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| Synonyms |
DU-176bDU 176 DU176DU-176bDU-176 Edoxaban Savaysa Lixiana
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~69.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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