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Purity: ≥98%
Edoxaban (also known as DU-176b; DU176; Lixiana; Savaysa) is a potent, direct-acting, selective, orally bioavailable factor Xa inhibitor used as an anticoagulant drug. It inhibits factor Xa with a Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa. Edoxaban acts as a direct factor Xa inhibitor. It 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. It has fewer drug interactions compared with warfarin.
| ln Vitro |
Human plasma's PT, TT, and APTT are prolonged by edoxaban in a concentration-dependent manner (1, 1, and 5 minutes, respectively)[1]. With an IC50 of 2.90 µM, edoxaban prevents platelet aggregation caused by thrombin[1].
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| ln Vivo |
Edoxaban prolongs PT and significantly and dose-dependently reduces thrombus formation at doses of 0.5, 2.5, and 12.5 mg/kg; po; once[1].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet Tested Concentrations: Incubation Duration: 1 and 5 minutes Experimental Results: Antithrombin. |
| Animal Protocol |
Animal/Disease Models: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model)[1].
Doses: 0.5, 2.5 and 12.5 mg/kg Route of Administration: Oral administration; once Experimental Results: Inhibited exogenous FXa activity. Antithrombotic. |
| 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 |
C24H30CLN7O4S
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| Molecular Weight |
548.06
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| CAS # |
480449-70-5
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| Related CAS # |
Edoxaban tosylate;480449-71-6;Edoxaban tosylate monohydrate;1229194-11-9;Edoxaban-d6;1304701-57-2;Edoxaban hydrochloride;480448-29-1
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| SMILES |
O=C(NC1=NC=C(Cl)C=C1)C(N[C@@H]2[ C@H](NC(C(S3)=NC4=C3CN(C)CC4)=O)C[C@@H](C(N(C)C)=O)CC2)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8246 mL | 9.1231 mL | 18.2462 mL | |
| 5 mM | 0.3649 mL | 1.8246 mL | 3.6492 mL | |
| 10 mM | 0.1825 mL | 0.9123 mL | 1.8246 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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