GlpBio

5-R-Rivaroxaban

目录号: GC11101纯度: >99.50%同义词: 5-R-利伐沙班
5-R-Rivaroxaban 是 Rivaroxaban 的 (R)-对映异构体。
5-R-Rivaroxaban
Cas No.: 865479-71-6
规格价格库存数量操作
5mg¥450.00现货
1
10mg¥630.00现货
1
25mg¥1,350.00现货
1
50mg¥2,520.00现货
1
100mg¥4,320.00现货
1
10mM (in 1mL DMSO)¥495.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Human, rabbit and rat plasma

Preparation method

The solubility of this compound in DMSO is >20.85mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

IC50: 21 nM (human and rabbit plasma)

Applications

Rivaroxaban competitively inhibited human FXa with the Ki value of 0.4 nM. Rivaroxaban inhibited prothrombinase activity with the IC50 of 2.1 nM. Rivaroxaban inhibited endogenous FXa more potently in human and rabbit plasma (IC50: 21 nM) than rat plasma (IC50:290 nM). Rivaroxaban demonstrated anticoagulant effects in human plasma, doubling prothrombin time (PT) and activated partial thromboplastin time at 0.23 and 0.69 μM, respectively.
Animal experiment [1,2]:

Animal models

Rat venous stasis model, Anaesthetised rat model

Dosage form

Intravenous inection, Oral administration, 2 mg/kg

Application

In a rat venous stasis model, Rivaroxaban (i.v.) dose-dependently reduced venous thrombosis with the ED50 of 0.1 mg/kg. Rivaroxaban (p.o.) reduced arterial (fibrin- and platelet-rich) thrombus formation in an arteriovenous (AV) shunt in rats (ED50: 5 mg/kg) and rabbits (ED50: 0.6 mg/kg). In anaesthetised rat model, pretreatment with 5-R-Rivaroxaban (i.v., 2 mg/kg) shortened bleeding time and clotting time.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Perzborn, E., Strassburger, J., Wilmen, A., Pohlmann, J., Roehrig, S., SCHLEMMER, K. H., & Straub, A. (2005). In vitro and in vivo studies of the novel antithrombotic agent BAY 59‐7939—an oral, direct Factor Xa inhibitor. Journal of Thrombosis and Haemostasis, 3(3), 514-521.

[2]. Perzborn, E., et al., Reversal of rivaroxaban anticoagulation by haemostatic agents in rats and primates. Thromb Haemost, 2013. 110(1): p. 162-72.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
865479-71-6
同义词
5-R-利伐沙班
化学名
5-chloro-N-[[(5R)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
SMILES
C1COCC(=O)N1C2=CC=C(C=C2)N3CC(OC3=O)CNC(=O)C4=CC=C(S4)Cl
分子式
C19H18ClN3O5S
分子量
435.88 g/mol
溶解性
≥ 20.85 mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol