N-[(1S,2R,4S)-4-carbamoyl-2-[(7-methyl-4,5,6,8-tetrahydropyrido[4,3-e][1,3]thiazine-2-carbonyl)amino]cyclohexyl]-N'-(5-chloropyridin-2-yl)oxamide,hydrochloride

Names

[ Name ]:
N-[(1S,2R,4S)-4-carbamoyl-2-[(7-methyl-4,5,6,8-tetrahydropyrido[4,3-e][1,3]thiazine-2-carbonyl)amino]cyclohexyl]-N'-(5-chloropyridin-2-yl)oxamide,hydrochloride

Biological Activity

[Description]:

Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin

Signaling Pathways >> Metabolic Enzyme/Protease >> Factor Xa

[Target]

IC50: 2.90 µM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa)[1]

[In Vitro]

Edoxaban hydrochloride (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner[1]. Edoxaban hydrochloride inhibits thrombin-induced platelet aggregation, with an IC50 of 2.90 µM[1]. Cell Viability Assay[1] Cell Line: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet Concentration: Incubation Time: 1 and 5 minutes Result: Antithrombin.

[In Vivo]

Edoxaban hydrochloride (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT[1]. Animal Model: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model)[1]. Dosage: 0.5, 2.5 and 12.5 mg/kg Administration: Oral administration; once Result: 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₉Cl₂N₇O₄S

[ Molecular Weight ]:
570.49200

[ Exact Mass ]:
569.13800

[ PSA ]:
185.17000

[ LogP ]:
2.84340

Related Compounds

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