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ximelagatran

Names

[ CAS No. ]:
192939-46-1

[ Name ]:
ximelagatran

[Synonym ]:
ximelagatran
ximelagatra
Ethyl N-{(1R)-1-cyclohexyl-2-[(2S)-2-{[4-(N-hydroxycarbamimidoyl)benzyl]carbamoyl}-1-azetidinyl]-2-oxoethyl}glycinate
Exanta
H-376/95
H 376-95
[14C]-Ximelagatran
Ethyl (((1R)-1-cyclohexyl-2-((2S)-2-((4-(hydroxycarbamimidoyl)benzyl)carbamoyl)azetidin-1-yl-2-oxoethyl)amino)acetate
H 376/95
[3H]-Ximelagatran
Ximelagatran (JAN/USAN/INN)
Exanta (TN)
Exarta
Ethyl N-{(1R)-1-cyclohexyl-2-[(2S)-2-{[4-(N'-hydroxycarbamimidoyl)benzyl]carbamoyl}azetidin-1-yl]-2-oxoethyl}glycinate
Glycine, N-[(1R)-1-cyclohexyl-2-[(2S)-2-[[[[4-[(hydroxyamino)iminomethyl]phenyl]methyl]amino]carbonyl]-1-azetidinyl]-2-oxoethyl]-, ethyl ester
Ximelagatran [USAN:INN]
ethyl 2-[[(1R)-1-cyclohexyl-2-[(2S)-2-[[4-[(Z)-N'-hydroxycarbamimidoyl]phenyl]methylcarbamoyl]azetidin-1-yl]-2-oxoethyl]amino]acetate

Biological Activity

[Description]:

Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin

[In Vitro]

Ximelagatran is an orally administered direct thrombin inhibitor under development as an anticoagulant agent for prophylaxis against and treatment of thromboembolism. Ximelagatran is rapidly absorbed and quickly converted into its active form Melagatran, a reversible, active-site inhibitor of both free and clot-bound thrombin that has stable and reproducible pharmacokinetic properties. Initial studies have shown Ximelagatran to have good efficacy and safety in the prevention of venous thromboembolism after total knee or total hip replacement[3].

[References]

[1]. Colwell CW Jr, et al. Comparison of ximelagatran, an oral direct thrombin inhibitor, with enoxaparin for the prevention of venous thromboembolism following total hip replacement. A randomized, double-blind study. J Thromb Haemost. 2003 Oct;1(10):2119-30.

[2]. Gao JH, et al. Effects of different anticoagulant drugs on the prevention of complications in patients after arthroplasty: A network meta-analysis. Medicine (Baltimore). 2017 Oct;96(40):e8059.

[3]. Francis CW, et al. Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement. N Engl J Med. 2003 Oct 30;349(18):1703-12.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C24H35N5O5

[ Molecular Weight ]:
473.565

[ Exact Mass ]:
473.263824

[ PSA ]:
143.85000

[ LogP ]:
2.08

[ Index of Refraction ]:
1.635

Related Compounds