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Edoxaban tosylate

Fxa inhibitor CAS# 480449-71-6

Edoxaban tosylate

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Chemical structure

Edoxaban tosylate

3D structure

Chemical Properties of Edoxaban tosylate

Cas No. 480449-71-6 SDF Download SDF
PubChem ID 44610678 Appearance Powder
Formula C31H38ClN7O7S2 M.Wt 720.26
Type of Compound N/A Storage Desiccate at -20°C
Synonyms DU-176b
Solubility 25℃: DMSO
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
SMILES CC1=CC=C(C=C1)S(=O)(=O)O.CN1CCC2=C(C1)SC(=N2)C(=O)NC3CC(CCC3NC(=O)C(=O)NC4=NC=C(C=C4)Cl)C(=O)N(C)C
Standard InChIKey ZLFZITWZOYXXAW-QXXZOGQOSA-N
Standard InChI InChI=1S/C24H30ClN7O4S.C7H8O3S/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)/t13-,15-,17+;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Edoxaban tosylate

DescriptionEdoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention IC50 Value: Target: factor Xa Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention in patients with atrial fibrillation, an elderly population that frequently receives aspirin (ASA) and/or nonsteroidal anti-inflammatory drugs for concurrent illnesses[1]. in vitro: Edoxaban PK was not affected by concomitant low-dose ASA or naproxen, but high-dose ASA increased systemic exposure of edoxaban by approximately 30%. The effects of edoxaban on prothrombin time, activated partial thromboplastin time, international normalized ratio, anti-FXa, and intrinsic FXa activity were not influenced by administration with ASA or naproxen. Inhibition of platelet aggregation by high-dose ASA, low-dose ASA, or naproxen was not affected by edoxaban[1]. in vivo: Forty-eight subjects, aged 18 to 45 years, received either edoxaban 60 mg once daily × 7 days (n = 24) or digoxin 0.25 mg twice daily × 2 days and once daily × 5 days (n = 24) and then concomitantly for 7 days. Serial blood and urine samples were collected for digoxin and edoxaban concentrations on days 7 and 14. Serial coagulation assays were measured for edoxaban on days 7 and 14. Edoxaban PK parameters demonstrated mild increases in area under the curve and peak concentrations of 9.5% and 15.6%, respectively[2], Clinical trial: Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans was reported[3].

References:
[1]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23. [Epub ahead of print] [2]. Mendell J, Noveck RJ, Shi M. Pharmacokinetics of the direct factor Xa inhibitor edoxaban and digoxin administered alone and in combination. J Cardiovasc Pharmacol. 2012 Oct;60(4):335-41. [3]. Bathala MS, Masumoto H, Oguma T, Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans. Drug Metab Dispos. 2012 Dec;40(12):2250-5.

Edoxaban tosylate Dilution Calculator

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Edoxaban tosylate Molarity Calculator

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Preparing Stock Solutions of Edoxaban tosylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.3884 mL 6.9419 mL 13.8839 mL 27.7678 mL 34.7097 mL
5 mM 0.2777 mL 1.3884 mL 2.7768 mL 5.5536 mL 6.9419 mL
10 mM 0.1388 mL 0.6942 mL 1.3884 mL 2.7768 mL 3.471 mL
50 mM 0.0278 mL 0.1388 mL 0.2777 mL 0.5554 mL 0.6942 mL
100 mM 0.0139 mL 0.0694 mL 0.1388 mL 0.2777 mL 0.3471 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Edoxaban tosylate

IC50 Value:N/A Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention in patients with atrial fibrillation, an elderly population that frequently receives aspirin (ASA) and/or nonsteroidal anti-inflammatory drugs for concurrent illnesses[1]. in vitro: Edoxaban PK was not affected by concomitant low-dose ASA or naproxen, but high-dose ASA increased systemic exposure of edoxaban by approximately 30%. The effects of edoxaban on prothrombin time, activated partial thromboplastin time, international normalized ratio, anti-FXa, and intrinsic FXa activity were not influenced by administration with ASA or naproxen. Inhibition of platelet aggregation by high-dose ASA, low-dose ASA, or naproxen was not affected by edoxaban[1]. in vivo: Forty-eight subjects, aged 18 to 45 years, received either edoxaban 60 mg once daily × 7 days (n = 24) or digoxin 0.25 mg twice daily × 2 days and once daily × 5 days (n = 24) and then concomitantly for 7 days. Serial blood and urine samples were collected for digoxin and edoxaban concentrations on days 7 and 14. Serial coagulation assays were measured for edoxaban on days 7 and 14. Edoxaban PK parameters demonstrated mild increases in area under the curve and peak concentrations of 9.5% and 15.6%, respectively[2], Clinical trial: Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans was reported[3].

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References on Edoxaban tosylate

Edoxaban tosylate.[Pubmed:21446778]

Am J Cardiovasc Drugs. 2011;11(2):129-35.

Daiichi Sankyo is developing Edoxaban tosylate (DU 176b; DU-176; DU-176b; DU176b) as an orally active direct factor Xa inhibitor for the prevention of stroke and the prevention and treatment of venous thromboembolism. Two dosing regimens of Edoxaban tosylate are being compared with warfarin over 24 months in the ENGAGE AF TIMI 48 trial (NCT00781391) in over 21 000 patients with atrial fibrillation in North and South America, Africa, Asia, Europe, Australia, and New Zealand. Edoxaban tosylate is also being compared with warfarin in the treatment and prevention of recurrent thromboembolic events in approximately 7500 patients with deep-vein thrombosis and/or pulmonary embolism in the HOKUSAI VTE trial (NCT00986154) being conducted in 40 countries. This review discusses the development history and scientific profile of this new compound.

Description

Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.

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