| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Edoxaban tosylate monohydrate (DU-176b; DU-176; trade name Lixiana), the tosylate salt of edoxaban which is a marketed anticoagulant drug, is a potent, selective, orally bioavailable and direct factor Xa inhibitor with potential anti-coagulant activity. 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 in a concentration-dependent manner by edoxaban monohydrate (1, 1, and 5 minutes) [1]. With an IC50 value of 2.90 μM, edoxaban monohydrate inhibits platelet aggregation produced by thrombin[1].
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| ln Vivo |
Edoxaban monohydrate prolongs prothrombin time (PT) and significantly and dose-dependently decreases thrombosis (0.5, 2.5, and 12.5 mg/kg; oral; 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. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because no information is available on the use of edoxaban during breastfeeding and the drug is orally absorbable, an alternate drug is preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Edoxaban tosylate hydrate is a hydrate that is the monohydrate of the tosylate salt of edoxaban. Used for the treatment of deep vein thrombosis and pulmonary embolism. It has a role as an anticoagulant, an EC 3.4.21.6 (coagulation factor Xa) inhibitor and a platelet aggregation inhibitor. It contains an edoxaban tosylate.
Drug Indication Prevention of stroke and systemic embolism in adult patients with nonvalvular atrial fibrillation (NVAF) with one or more risk factors, such as congestive heart failure, hypertension, age ⥠75 years, diabetes mellitus, prior stroke or transient ischaemic attack (TIA). Treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE), and prevention of recurrent DVT and PE in adults. |
| Molecular Formula |
C24H30CLN7O4S.C7H8O3S.H2O
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|---|---|
| Molecular Weight |
738.27
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| Exact Mass |
737.206
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| CAS # |
1229194-11-9
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| Related CAS # |
Edoxaban;480449-70-5;Edoxaban tosylate;480449-71-6;Edoxaban hydrochloride;480448-29-1
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| PubChem CID |
25022378
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| Appearance |
White to off-white solid powder
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| LogP |
4.34
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
49
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CN1CCC2=C(C1)SC(=N2)C(=O)N[C@@H]3C[C@H](CC[C@@H]3NC(=O)C(=O)NC4=NC=C(C=C4)Cl)C(=O)N(C)C.O
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| InChi Key |
PSMMNJNZVZZNOI-SJILXJHISA-N
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| InChi Code |
InChI=1S/C24H30ClN7O4S.C7H8O3S.H2O/c1-31(2)24(36)13-4-6-15(27-20(33)21(34)30-19-7-5-14(25)11-26-19)17(10-13)28-22(35)23-29-16-8-9-32(3)12-18(16)37-23;1-6-2-4-7(5-3-6)11(8,9)10;/h5,7,11,13,15,17H,4,6,8-10,12H2,1-3H3,(H,27,33)(H,28,35)(H,26,30,34);2-5H,1H3,(H,8,9,10);1H2/t13-,15-,17+;;/m0../s1
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| Chemical Name |
N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide;4-methylbenzenesulfonic acid;hydrate
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| Synonyms |
DU176b; DU 176b; Edoxaban; DU-176; DU 176; DU-176b; DU176; Edoxaban tosylate monohydrate, trade name Lixiana.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.39 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 (3.39 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 (3.39 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 | 1.3545 mL | 6.7726 mL | 13.5452 mL | |
| 5 mM | 0.2709 mL | 1.3545 mL | 2.7090 mL | |
| 10 mM | 0.1355 mL | 0.6773 mL | 1.3545 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02801669 | Completed Has Results | Drug: Du-176b Drug: placebo |
Atrial Fibrillation | Daiichi Sankyo Co., Ltd | August 5, 2016 | Phase 3 |
| NCT01857622 | Completed Has Results | Drug: DU-176b 15mg Drug: DU-176b 30mg |
Non-valvular Atrial Fibrillation | Daiichi Sankyo Co., Ltd. | November 2011 | Phase 3 |
| NCT01181141 | Completed Has Results | Drug: DU-176b (edoxaban) Drug: Enoxaparin sodium 20mg |
Venous Thromboembolism | Daiichi Sankyo Co., Ltd. | October 2008 | Phase 3 |
| NCT01203098 | Completed Has Results | Drug: DU-176b 15mg Drug: DU-176b 30mg |
Venous Thromboembolism Thromboembolism |
Daiichi Sankyo Co., Ltd. | July 2008 | Phase 2 |
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