Home >> Research Area >>Proteases/Proteasome>>Thrombin>> Edoxaban tosylate monohydrate

Edoxaban tosylate monohydrate

Oral factor Xa inhibitor CAS# 1229194-11-9

Edoxaban tosylate monohydrate

Catalog No. BCC1545----Order now to get a substantial discount!

Product Name & Size Price Stock
Edoxaban tosylate monohydrate: 5mg $81 In Stock
Edoxaban tosylate monohydrate: 10mg Please Inquire In Stock
Edoxaban tosylate monohydrate: 20mg Please Inquire Please Inquire
Edoxaban tosylate monohydrate: 50mg Please Inquire Please Inquire
Edoxaban tosylate monohydrate: 100mg Please Inquire Please Inquire
Edoxaban tosylate monohydrate: 200mg Please Inquire Please Inquire
Edoxaban tosylate monohydrate: 500mg Please Inquire Please Inquire
Edoxaban tosylate monohydrate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Edoxaban tosylate monohydrate

Number of papers citing our products

Chemical structure

Edoxaban tosylate monohydrate

3D structure

Chemical Properties of Edoxaban tosylate monohydrate

Cas No. 1229194-11-9 SDF Download SDF
PubChem ID 25022378 Appearance Powder
Formula C31H40ClN7O8S2 M.Wt 738.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (67.73 mM; Need ultrasonic)
H2O : 1 mg/mL (1.35 mM; Need ultrasonic)
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
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.O
Standard InChIKey PSMMNJNZVZZNOI-SJILXJHISA-N
Standard InChI 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
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 monohydrate

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 monohydrate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Edoxaban tosylate monohydrate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Edoxaban tosylate monohydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.3545 mL 6.7726 mL 13.5452 mL 27.0904 mL 33.8629 mL
5 mM 0.2709 mL 1.3545 mL 2.709 mL 5.4181 mL 6.7726 mL
10 mM 0.1355 mL 0.6773 mL 1.3545 mL 2.709 mL 3.3863 mL
50 mM 0.0271 mL 0.1355 mL 0.2709 mL 0.5418 mL 0.6773 mL
100 mM 0.0135 mL 0.0677 mL 0.1355 mL 0.2709 mL 0.3386 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.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Edoxaban tosylate monohydrate

Factor Xa (FXa), a key serine protease, is a promising target enzyme for the prophylaxis and treatment of thromboembolic diseases. Edoxaban tosylate monohydrate is a novel antithrombotic agent that directly inhibits FXa activity.

In vitro: Edoxaban tosylate monohydrate (DU-176b) inhibited FXa with Ki values of 0.561 nM for free FXa, 2.98 nM for prothrombinase, and exhibited >10 000-fold selectivity for FXa. DU-176b doubled prothrombin time and activated partial thromboplastin time in human plasma. DU-176b did not impair platelet aggregation by ADP, collagen or U46619 [1].

In vivo: DU-176b dose-dependently inhibited thrombus formation in rat and rabbit thrombosis models, although bleeding time in rats was not significantly prolonged at an antithrombotic dose [1].

Clinical trial: A previous study determined the mass balance and pharmacokinetics of edoxaban in humans after oral administration of [14C]edoxaban. The mass balance of edoxaban study showed unchanged edoxaban as the most abundant component. Edoxaban was eliminated through multiple pathways, but each accounts for only a small amount of overall elimination [2].

References:
[1] Furugohri T, Isobe K, Honda Y, Kamisato-Matsumoto C, Sugiyama N, Nagahara T, Morishima Y, Shibano T.  DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008;6(9):1542-9.
[2] Bathala MS, Masumoto H, Oguma T, He L, Lowrie C, Mendell J.  Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans. Drug Metab Dispos. 2012;40(12):2250-5.

Featured Products
New Products
 

Description

Edoxaban tosylate monohydrate (DU-176b monohydrate) 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 monohydrate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate monohydrate 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 monohydrate has antithrombotic properties and has potential for thromboembolic diseases treatment.

Keywords:

Edoxaban tosylate monohydrate,1229194-11-9,Natural Products,Thrombin, buy Edoxaban tosylate monohydrate , Edoxaban tosylate monohydrate supplier , purchase Edoxaban tosylate monohydrate , Edoxaban tosylate monohydrate cost , Edoxaban tosylate monohydrate manufacturer , order Edoxaban tosylate monohydrate , high purity Edoxaban tosylate monohydrate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: