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Edoxaban tosylate monohydrate

Catalog No.
A3383
Oral factor Xa inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
5mg
$61.00
In stock
10mg
$85.00
In stock
50mg
$157.00
In stock
200mg
$429.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt738.27
Cas No.1229194-11-9
FormulaC31H40ClN7O8S2
Solubility≥36.91 mg/mL in DMSO; insoluble in H2O; ≥5.78 mg/mL in EtOH with gentle warming and ultrasonic
Chemical NameN'-(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
SDFDownload SDF
Canonical SMILESCC1=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
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

Edoxaban tosylate monohydrate