Rivaroxaban
Based on 16 publication(s) in Google Scholar
Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 366789-02-8
- Formula: C19H18ClN3O5S
- Molecular Weight:435.88
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Rivaroxaban
More- Elife. 2022 Mar 23:11:e77444. [Abstract]
- Pharmaceutics. 2019 Mar 19;11(3). pii: E133. [Abstract]
- Int J Mol Sci. 2021 Mar 24;22(7):3323. [Abstract]
- Molecules. 2023 Feb 28;28(5):2254. [Abstract]
- J Pharm Sci. 2017 Sep;106(9):2524-2534. [Abstract]
- Res Pract Thromb Haemost. 2020 Oct 25;4(8):1269-1281. [Abstract]
- Thromb Res. 2016 Jul:143:28-33. [Abstract]
- Platelets. 2020 Aug 7;1-8. [Abstract]
- BMC Cardiovasc Disord. 2023 Jun 2;23(1):282. [Abstract]
- Int J Lab Hematol. 2020 Apr;42(2):126-133. [Abstract]
- Drug Metab Pharmacokinet. 2023 Dec:53:100498. [Abstract]
- Biomed Chromatogr. 2022 May;36(5):e5306. [Abstract]
- LabMed. 2024 Nov 18.
- Chemical Methodologies. 2026 Jan;10(3):253-273.
- University of Bonn. 2023 May 31.
- Patent. US20170224812A1.
Customer Validation & Images
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Cell Migration/Invasion Assay
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Cell Migration/Invasion Assay
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ELISA
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PK/PD Analysis
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Bio/Physico-chemical Assay
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| Platelet | EC50 |
>10 μM
Compound: Rivaroxaban
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Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
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[PMID: 36462436] |
| Platelet | EC50 |
0.01 μM
Compound: Rivaroxaban
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Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
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[PMID: 36462436] |
Rivaroxaban (BAY 59-7939) is an oral, direct Factor Xa (FXa) inhibitor in development for the prevention and treatment of arterial and venous thrombosis. Rivaroxaban competitively inhibits human FXa (Ki 0.4 nM) with >10 000-fold greater selectivity than for other serine proteases; it also inhibits prothrombinase activity (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa more potently in human and rabbit plasma (IC50 21 nM) than rat plasma (IC50 290 nM). It demonstrates anticoagulant effects in human plasma, doubling prothrombin time (PT) and activates partial thromboplastin time at 0.23 and 0.69 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 366789-02-8
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Appearance Solid
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Molecular Weight 435.88
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Formula C19H18ClN3O5S
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Color White to off-white
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SMILES
O=C(N(C1=CC=C(N2C(COCC2)=O)C=C1)C3)O[C@H]3CNC(C4=CC=C(S4)Cl)=O
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Synonyms
BAY 59-7939
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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Elife
2022 Mar 23:11:e77444. PMID: 35294338 -
Pharmaceutics
Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban. [Abstract]2019 Mar 19;11(3). pii: E133. PMID: 30893910
Rivaroxaban purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2019 Mar 19;11(3). pii: E133. [Abstract]
Pharmacokinetic parameters of rivaroxaban following an oral administration of Rivaroxaban (2 mg/kg) in the presence, or absence, of either verapamil (25 mg/kg) or diltiazem (30 mg/kg) (mean (relative standard deviation, %), n = 5).
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Int J Mol Sci
A Combined Activity of Thrombin and P-Selectin Is Essential for Platelet Activation by Pancreatic Cancer Cells. [Abstract]2021 Mar 24;22(7):3323. PMID: 33805059 -
Molecules
Generic Methods for Simultaneous Analysis of Four Direct Oral Anticoagulants in Human Plasma and Urine by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry. [Abstract]2023 Feb 28;28(5):2254. PMID: 36903499 -
J Pharm Sci
Different Involvement of OAT in Renal Disposition of Oral Anticoagulants Rivaroxaban, Dabigatran, and Apixaban. [Abstract]2017 Sep;106(9):2524-2534. PMID: 28456731
Rivaroxaban purchased from MedChemExpress. Usage Cited in: J Pharm Sci. 2017 Sep;106(9):2524-2534. [Abstract]
Rivaroxaban showed significant inhibitory effects on hOAT3, with an IC50 value of 8.2 μM in HEK293 cells.
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Res Pract Thromb Haemost
Effect of anticoagulants on fibrin clot structure: A comparison between vitamin K antagonists and factor Xa inhibitors. [Abstract]2020 Oct 25;4(8):1269-1281. PMID: 33313466 -
Thromb Res
Bidirectional functions of thrombin on fibrinolysis: Evidence of thrombin-dependent enhancement of fibrinolysis provided by spontaneous plasma clot lysis. [Abstract]2016 Jul:143:28-33. PMID: 27179129 -
Platelets
Factor Xa and thrombin induce endothelial progenitor cell activation. The effect of direct oral anticoagulants. [Abstract]2020 Aug 7;1-8. PMID: 32762584
Rivaroxaban purchased from MedChemExpress. Usage Cited in: Platelets. 2020 Aug 7;1-8. [Abstract]
The effect of rivaroxaban and dabigatran on FXa- and thrombin-induced ICAM-1 expression on OECs and HUVECs. Cells were incubated for 10 min with 10 μM Rivaroxaban or 20 μM dabigatran and then were activated with 50 nM FXa or 80 nM thrombin for 24 h, respectively. The results showed that Rivaroxaban (Riva) dose-dependently inhibited FXa-induced ICAM-1 expression in OECs, with the inhibition rate ranging from 4% at 0.1 μM to 94% at 20 μM. Rivaroxaban also exerted a dose-dependent suppressive effect on FXa-stimulated ICAM-1 expression in HUVECs. The inhibition rate was 9% at 1 μM and reached 95% at 10 μM.
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BMC Cardiovasc Disord
Effects of the factor Xa inhibitor rivaroxaban on the differentiation of endothelial progenitor cells. [Abstract]2023 Jun 2;23(1):282. PMID: 37268884
Rivaroxaban purchased from MedChemExpress. Usage Cited in: BMC Cardiovasc Disord. 2023 Jun 2;23(1):282. [Abstract]
EPCs exposed to 0.1% DMSO (control) or rivaroxaban for 7 days were cultured for 6 h. Rivaroxaban (1 μM; 7 days) significantly enhanced the adhesion capacity of EPCs.
Rivaroxaban purchased from MedChemExpress. Usage Cited in: BMC Cardiovasc Disord. 2023 Jun 2;23(1):282. [Abstract]
EPCs exposed to 0.1% DMSO (control) or Rivaroxaban for 7 days were cultured in Matrigel with human umbilical vein endothelial cells. Rivaroxaban (0.1 μM; 7 days) enhanced the tubule formation capacity of EPCs.
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Int J Lab Hematol
Differential effects of direct factor IIa and factor Xa inhibitors in protein C-deficient plasma detected using thrombin generation and viscoelastometry assays. [Abstract]2020 Apr;42(2):126-133. PMID: 31756037 -
Drug Metab Pharmacokinet
Involvement of multiple cytochrome P450 isoenzymes in drug interactions between ritonavir and direct oral anticoagulants. [Abstract]2023 Dec:53:100498. PMID: 37778107 -
Biomed Chromatogr
Developing LC-MS/MS methods to quantify rivaroxabanin human plasma and urine: Application to therapeutic drug monitoring. [Abstract]2022 May;36(5):e5306. PMID: 34967030 -
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Solvent & Solubility
DMSO : 50 mg/mL (114.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.74 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The activity of Rivaroxaban (BAY 59-7939) against purified serine proteases is measured using chromogenic or fluorogenic substrates in 96-well microtiter plates at 25°C. The enzymes are incubated with Rivaroxaban or its solvent, DMSO, for 10 min. The reactions are initiated by the addition of the substrate, and the color or fluorescence is monitored continuously at 405 nm using a Spectra Rainbow Thermo Reader, or at 630/465 nm using a SPECTRAfluor plus, respectively, for 20 min. Enzymatic activity is analyzed in the following buffers (final concentrations): human FXa (0.5 nM), rabbit FXa (2 nM), rat FXa (10 nM), or urokinase (4 nM) in 50 mM Tris-HCl buffer, pH 8.3, 150 mM NaCl, and 0.1% bovine serum albumin (BSA); Pefachrome FXa (50-800 μM) or chromozym U (250 μM) with thrombin (0.69 nM), trypsin (2.2 nM), or plasmin (3.2 nM) in 0.1 μM Tris-HCl, pH 8.0, and 20 mM CaCl2; chromozym TH (200 μM), chromozym plasmin (500 μM), or chromozymtrypsin (500 μM) with FXIa (1 nM) or APC (10 nM) in 50mM phosphate buffer, pH 7.4, 150 mM NaCl; and S 2366 (150 or 500 μM) with FVIIa (1 nM) and tissue factor (3 nM) in 50 mM Tris-HCl buffer, pH 8.0, 100 mM NaCl, 5 mM CaCl2 and 0.3% BSA, H-D-Phe-Pro-Arg-6-amino-1-naphthalene-benzylsulfon-amide H2O (100 μM) and measured for 3 h. The FIXab/FX assay, comprising FIXab (8.8 nM) and FX (9.5 nM) in 50 mM Tris-HCl buffer, pH 7.4, 100 mM NaCl, 5 mM CaCl2 and 0.1% BSA, is started by the addition of I-1100 (50 μM), and measured for 60 min. The inhibitory constant (Ki) against FXa is calculated according to the Cheng-Prusoff equation (Ki=IC50/1+[S]/Km), where [S] is the substrate concentration, and Km is the Michaelis-Menten constant. Km is determined from a Lineweaver-Burk plot. The IC50 is the amount of inhibitor required to diminish the initial velocity of the control by 50%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
Fasted, male Wistar rats (HsdCpb:WU) are used. Rat venous stasis model Thrombus formation is induced in anesthetized rats (n=10 per dose group), with minor modifications. The abdominal vena cava is exposed and two loose sutures (8-10 mm apart) are placed below the left renal venous branch. Rivaroxaban dissolved in polyethylene glycol/H2O/glycerol (996 g/100 g/60 g), or vehicle is given by intravenous (i.v.) bolus injection into a tail vein 15 min before thrombus induction. Thromboplastin (0.5 mg/kg) is injected into a femoral vein and, after 15 s, the proximal and distal sutures are tied. Fifteen minutes later, the ligated segment is removed, the thrombus withdrawn and weighed. Blood samples are obtained by cardiac puncture immediately before thrombus removal.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Roehrig S, et al. Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. J Med Chem. 2005 Sep 22;48(19) [Content Brief]
[2]. Perzborn E, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor. J Thromb Haemost. 2005 Mar;3(3):514-21. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2942 mL | 11.4710 mL | 22.9421 mL | 57.3552 mL |
| 5 mM | 0.4588 mL | 2.2942 mL | 4.5884 mL | 11.4710 mL | |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2942 mL | 5.7355 mL | |
| 15 mM | 0.1529 mL | 0.7647 mL | 1.5295 mL | 3.8237 mL | |
| 20 mM | 0.1147 mL | 0.5736 mL | 1.1471 mL | 2.8678 mL | |
| 25 mM | 0.0918 mL | 0.4588 mL | 0.9177 mL | 2.2942 mL | |
| 30 mM | 0.0765 mL | 0.3824 mL | 0.7647 mL | 1.9118 mL | |
| 40 mM | 0.0574 mL | 0.2868 mL | 0.5736 mL | 1.4339 mL | |
| 50 mM | 0.0459 mL | 0.2294 mL | 0.4588 mL | 1.1471 mL | |
| 60 mM | 0.0382 mL | 0.1912 mL | 0.3824 mL | 0.9559 mL | |
| 80 mM | 0.0287 mL | 0.1434 mL | 0.2868 mL | 0.7169 mL | |
| 100 mM | 0.0229 mL | 0.1147 mL | 0.2294 mL | 0.5736 mL |
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