865479-71-6 Usage
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 865479-71-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,5,4,7 and 9 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 865479-71:
(8*8)+(7*6)+(6*5)+(5*4)+(4*7)+(3*9)+(2*7)+(1*1)=226
226 % 10 = 6
So 865479-71-6 is a valid CAS Registry Number.
865479-71-6Relevant articles and documents
Preparation method of rivaroxaban
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Paragraph 0008; 0017; 0019-0020; 0022-0023; 0025-0026; 0028, (2021/03/18)
The invention relates to a preparation method of rivaroxaban, belongs to the field of medicines, particularly relates to a preparation method for efficiently synthesizing rivaroxaban by taking 5-chlorothiophene-2-amide as a raw material through four steps of Boc protection, substitution reaction, cyclization reaction and deprotection reaction. The preparation method has few steps, less three wastes and good product purity.
Preparation method of rivaroxaban
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, (2021/01/25)
The invention relates to a preparation method of rivaroxaban, in particular to a method for efficiently synthesizing rivaroxaban by taking p-nitroaniline and (S)-N-glycidol phthalimide as raw materials through seven steps: an addition reaction, a cyclization reaction, a hydrolysis reaction, an amidation reaction, a reduction reaction, an addition reaction and a cyclization reaction. The provided rivaroxaban preparation method has the advantages of high yield, low cost, few three wastes, and high product purity and is suitable for industrialization.
A Convenient Synthesis of Rivaroxaban from (S)-Epichlorohydrin
Halama, Ale?,Kruli?, Radim,Ryme?, Jan
, (2020/04/27)
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