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Zifaxaban

Names

[ CAS No. ]:
1378266-98-8

[ Name ]:
Zifaxaban

[Synonym ]:
5-Chloro-N-({(5S)-2-oxo-3-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
2-Thiophenecarboxamide, 5-chloro-N-[[(5S)-2-oxo-3-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-5-oxazolidinyl]methyl]-

Biological Activity

[Description]:

Zifaxaban is a novel, potent, selective, direct and oral factor Xa inhibitor with IC50 of 11.1 nM (human FXa), displays > 10,000-fold selectivity than other serine proteases; also deoes not impair platelet aggregation induced by collagen, adenosine diphosphate (ADP) or arachidonic acid; significantly prolongs clotting time, prothrombin time (PT), and activated partial thromboplastin time (APTT) in the plasma of humans, rabbits, and rats, with a relatively weak effect on thrombin time; strongly suppresses thrombus formation with ED50 values of 3.09 mg/kg in venous thrombosis models in rats.

[References]

References 1. Qiu X, et al. Eur J Pharmacol. 2018 Aug 17. pii: S0014-2999(18)30469-2. View Related Products by Target Factor Xa

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
680.2±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C20H16ClN3O4S

[ Molecular Weight ]:
429.877

[ Flash Point ]:
365.2±31.5 °C

[ Exact Mass ]:
429.054993

[ LogP ]:
2.45

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.663

Related Compounds