Art. -Nr.: HY-50903

Rivaroxaban

Name: Rivaroxaban
Brand: MedChemExpress
SKU: HY-50903
Price: 60.00 USD
Availability: InStock
Rating: 5 (16 reviews)

(Synonyms: BAY 59-7939)

16 Cited Publications

Kundenbewertung

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; K_i 0.4 nM).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.93%
CAS. Nr.: 366789-02-8
Formel: C₁₉H₁₈ClN₃O₅S
Molecular Weight:435.88

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Rivaroxaban Chemical Structure

CAS. Nr.: 366789-02-8

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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; K_i 0.4 nM)^[1]^[2].

IC₅₀ & Target

IC50: 0.7 nM (FXa)^[1]
Ki: 0.4 nM (FXa)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	EC₅₀	>10 μM Compound: Rivaroxaban	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	[PMID: 36462436]
Platelet	EC₅₀	0.01 μM Compound: Rivaroxaban	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	[PMID: 36462436]

In Vitro

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 (K_i 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.

In Vivo

Rivaroxaban (BAY 59-7939) is a potent and selective, direct FXa inhibitor with excellent in vivo activity and good oral bioavailability^[1]. Rivaroxaban (BAY 59-7939), administered by i.v. bolus before thrombus induction, reduces thrombus formation (ED₅₀ 0.1 mg/kg), inhibits FXa, and prolongs PT dose dependently. PT and FXa are affected slightly at the ED₅₀ (1.8-fold increase and 32% inhibition, respectively). At 0.3 mg/kg (dose leading to almost complete inhibition of thrombus formation), Rivaroxaban moderately prolongs PT (3.2±0.5-fold) and inhibits FXa activity (65±3%)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 366789-02-8
Appearance Solid
Molecular Weight 435.88
Formel C₁₉H₁₈ClN₃O₅S
Color White to off-white
SMILES

O=C(N(C1=CC=C(N2C(COCC2)=O)C=C1)C3)O[C@H]3CNC(C4=CC=C(S4)Cl)=O
Synonyms

BAY 59-7939
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (16)

All PK/PD AnalysisBio/Physico-chemical AssayELISACell Migration/Invasion Assay

Sort by:

Journal Impact Factor

Pharmaceutics

Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban. [Abstract]

2019 Mar 19;11(3):133. PMID: 30893910

Rivaroxaban purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2019 Mar 19;11(3):133. [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).
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.
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
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.
Platelets

Factor Xa and thrombin induce endothelial progenitor cell activation. The effect of direct oral anticoagulants. [Abstract]

2021 Aug 18;32(6):807-814. PMID: 32762584

Rivaroxaban purchased from MedChemExpress. Usage Cited in: Platelets. 2021 Aug 18;32(6):807-814. [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.
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
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
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
LabMed

2024 Nov 18.
Chemical Methodologies

2026 Jan;10(3):253-273.
University of Bonn

2023 May 31.
Elife

Coagulation factors directly cleave SARS-CoV-2 spike and enhance viral entry. [Abstract]

2022 Mar 23:11:e77444. PMID: 35294338
Patent

US20170224812A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2942 mL

11.4710 mL

22.9421 mL

5 mM

0.4588 mL

2.2942 mL

4.5884 mL

10 mM

0.2294 mL

1.1471 mL

2.2942 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[2]

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 (K_i) against FXa is calculated according to the Cheng-Prusoff equation (K_i=IC₅₀/1+[S]/K_m), where [S] is the substrate concentration, and K_m is the Michaelis-Menten constant. K_m 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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Bioz

Keywords

Rivaroxaban

16 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Rivaroxaban

Publications Citing Use of MedChemExpress (MCE) Rivaroxaban