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KI3515BAY 59-7939QuoteQuote

Chemical Characteristic

Product NameBAY 59-7939
SynonymsRivaroxaban, Xarelto
CAS No.366789-02-8
Molecular Weight 435.88
FormulaC19H18ClN3O5S
Chemical Name(S)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide
Smilesc1(ccc(s1)Cl)C(=O)NCC1OC(=O)N(C1)c1ccc(cc1)N1C(=O)COCC1
Chemical Structure

Biological activities

BAY 59-7939 is a direct inhibitor of factor Xa. BAY 59-7939 is a novel, oral anticoagulant for the prevention and treatment of thromboembolic disorders.[1] BAY 59-7939 inhibits prothrombinase complex-bound and clot-associated factor Xa with IC50s of 2.1 and 75 nM, respectively. BAY 59-7939 shows a strong affinity to purified human, rabbit and rat factor Xa with IC50s of 0.7, 0.8 and 3.4 nM, respectively. BAY 59-7939 inhibits factor Xa in a concentration-dependent manner with a Ki of 0.4 nM. In vitro, BAY 59-7939 prolongs the initiation phase of thrombin generation and reduces the thrombin burst produced in the propagation phase. BAY 59-7939 effectively and concentration-dependently inhibits tissue factor-induced platelet aggregation by the inhibition of thrombin generation with an IC50 of 60 nM in defibrinated plasma. In vivo, in a rabbit thrombosis model, BAY 59-7939 also inhibits thrombus growth of preformed clots in the jugular vein. BAY 59-7939 shows effective dose-dependent antithrombotic activity in arterial (fibrin-poor and platelet-rich) thrombosis models, such as the arteriovenous shunt model in rats and rabbits.[2]

Protocols

In vivo, BAY 59-7939 is dissolved in water.[2]

References

[1] Kubitza D, et al. Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939--an oral, direct Factor Xa inhibitor--after multiple dosing in healthy male subjects. Eur J Clin Pharmacol. 2005, 61(12): 873-880.
[2] Perzborn E, Rivaroxaban: a new oral factor Xa inhibitor. Arterioscler Thromb Vasc Biol. 2010, 30(3): 376-381.

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