Identification | Back Directory | [Name]
5-R-Rivaroxaban | [CAS]
865479-71-6 | [Synonyms]
R-Rivaroxaban Rivaroxaban A Rivaroxaban-6 5-R-Rivaroxaban ent-Rivaroxaban Rivaroxaban R-Isomer XARELTO; BAY 59-7939 Rivaroxyban R-isomer R-Rivaroxaban Impurity R-ENANTIOMER OF RIVAROXABAN Rivaroxaban R-Isomer Impurity (R)-Rivaroxaban, ent-Rivaroxaban Rivaroxaban R-Isomer (ent-Rivaroxaban) Rivaroxaban impurity H: 5-R Rivaroxaban Rivaroxaban Impurity 6(Rivaroxaban R-Isomer) Rivaroxaban EP Impurity A/Rivaroxaban R-isomer Impurity (R)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide (S)-4-(4-(5-(((2-methyl-4-oxopentan-2-yl)amino)methyl)-2- oxooxazolidin-3-yl)phenyl)morpholin-3-one 5-Chloro-N-[[(5R)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide 2-Thiophenecarboxamide, 5-chloro-N-[[(5R)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]- Rivaroxaban impurity 7/5-R-Rivaroxaban/ent-Rivaroxaban/5-Chloro-N-[[(5R)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide | [Molecular Formula]
C19H18ClN3O5S | [MDL Number]
MFCD17171369 | [MOL File]
865479-71-6.mol | [Molecular Weight]
435.88 |
Chemical Properties | Back Directory | [Melting point ]
>227°C (dec.) | [Boiling point ]
732.6±60.0 °C(Predicted) | [density ]
1.460 | [storage temp. ]
Refrigerator | [solubility ]
Acetonitrile (Slightly, Heated, Sonicated), DMSO (Slightly, Sonicated), Methanol | [form ]
Solid | [pka]
13.36±0.46(Predicted) | [color ]
White to Off-White |
Hazard Information | Back Directory | [Uses]
ent-Rivaroxaban is the R-isomer of Rivaroxaban (R538000), which is a novel antithrombotic agent. A highly potent and selective, direct FXa inhibitor. | [Biological Activity]
5-r-rivaroxaban is a selective inhibitor of human factor xa with ic50 value of 0.7 nmol/l [1].factor xa is a serine endopeptidase enzyme and plays an important role in the convergence point of the intrinsic and extrinsic pathways in blood coagulation system [2].5-r-rivaroxaban is an oral, direct factor xa inhibitor and the inhibition is species-dependent. when tested with purified factoe xa from human or rabbit, 5-r-rivaroxaban showed similar affinity with ic50 value of 0.7 nmol/l and 0.8 nmol/l, respectively, while had a ic50 value as low as 3.4 nmol/l when tested with rat factor xa [1].pre-treated anaesthetised rat model with intravenous 5-r-rivaroxaban at a dose of 2 mg/kg, and after bleeding initiated intravenous treated with rfviia (100/400 μg/kg), pcc (25/50 u/kg) or apcc (50/100 u/kg), the result showed that 5-r-rivaroxaban pre-treatment significantly shorten bleeding time and clotting time compared with 5-r-rivaroxaban alone treated group [2]. similar results were obtained when tested with rabbit model [1].it has been reported that 5-r-rivaroxaban is a promising drug for atrial fibrillation, venous thromboembolism or thromboembolic disorders in clinic [3] [4] [1]. | [storage]
Store at -20°C | [References]
[1]. perzborn, e., et al., rivaroxaban: a new oral factor xa inhibitor. arterioscler thromb vasc biol, 2010. 30(3): p. 376-81. [2]. perzborn, e., et al., reversal of rivaroxaban anticoagulation by haemostatic agents in rats and primates. thromb haemost, 2013. 110(1): p. 162-72. [3]. beyer-westendorf, j., et al., efficacy and safety of rivaroxaban or fondaparinux thromboprophylaxis in major orthopedic surgery: findings from the ortho-tep registry. j thromb haemost, 2012. 10(10): p. 2045-52. [4]. palareti, g., et al., clinical management of rivaroxaban-treated patients. expert opin pharmacother, 2013. 14(5): p. 655-67. |
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