Rivaroxaban

Catalog No.S3002 Synonyms: BAY 59-7939

Rivaroxaban Chemical Structure

Molecular Weight(MW): 435.88

Rivaroxaban is a direct inhibitor of Factor Xa with Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively. It is selective for human factor Xa, for which it has >10 000-fold greater selectivity than for other biologically relevant serine proteases (IC50 >20 μM).

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 170 In stock
USD 270 In stock
USD 870 In stock
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1 Customer Review

  • In vivo, scatter plot of PT (a)、PT ratio(b)、APTT(c) and APTT ratio(d) versus rivaroxaban concentrations measured by Biophen DiXaI. Biophen DiXaI, Biophen Direct Factor Xa Inhibitor; PT, prothrombin time; PT ratios, prothrombin time versus the normal pooled plasma (NPP); APTT, activated partial thromboplastin time; APTT ratios, activated partial thromboplastin time versus NPP.

    Br J Biomed Sci, 2016, 73(3):134-139.. Rivaroxaban purchased from Selleck.

Purity & Quality Control

Choose Selective Factor Xa Inhibitors

Biological Activity

Description Rivaroxaban is a direct inhibitor of Factor Xa with Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively. It is selective for human factor Xa, for which it has >10 000-fold greater selectivity than for other biologically relevant serine proteases (IC50 >20 μM).
Targets
Factor Xa [1]
(Cell-free assay)
Prothrombinase [1]
(Cell-free assay)
0.7 nM 2.1 nM
In vitro

Rivaroxaban is an oral, direct inhibitor of Factor Xa (FXa), being developed for the prevention and treatment of arterial and venous thrombosis with a Ki of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity with IC50 of 2.1 nM. Rivaroxaban also shows a similar affinity to purified human and rabbit FXa (IC50 0.7 nM and 0.8 nM, respectively), but a lesser potency against purified rat FXa (IC50 3.4 nM). Endogenous human and rabbit FXa in plasma is inhibited to a similar extent by Rivaroxaban (IC50 21 nM and 21 nM, respectively), while 14-fold higher concentrations are required in rat plasma (IC50 290 nM). [1] Rivaroxaban exhibits high permeability and polarized transport across Caco-2 cells as a substrate of the P-gp, but exhibits no inhibitory effect on P-gp-mediated drug transport up to concentrations of 100 μM in vitro. [2]

In vivo Rivaroxaban reduces venous thrombosis in a dose dependent manner (ED50 0.1 mg/kg i.v.) in a rat venous stasis model. Rivaroxaban reduces arterial thrombus formation in an arteriovenous (AV) shunt in rats (ED50 5.0 mg/kg p.o.) and rabbits (ED50 0.6 mg/kg p.o.). [1] Plasma pharmacokinetics of Rivaroxaban are linear across the investigated dose range (1-10 mg/kg in rats, 0.3-3 mg/kg in dogs). Plasma clearance is low: 0.4 L/kg/h in rats and 0.3 L/kg/h in dogs; the volume of distribution (V(ss)) is moderate: 0.3 L/kg in rats, and 0.4 L/kg in dogs. The elimination half-life after oral administration is short in both species (0.9-2.3 hours). [3]

Protocol

Kinase Assay:

[1]

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Factor Xa Activity :

The activity of Rivaroxaban against purified serine proteases is measured using chromogenic or fluorogenic substrates in 96-well microtiter plates. The enzymes are incubated with Rivaroxaban or its solvent, dimethyl sulfoxide (DMSO), for 10 minutes. 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 minutes. 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 chromozym trypsin (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-benzylsulfonamide-H2O (100 μM) and measured for 3 hours. The FIXaβ/FX assay, comprising FIXaβ (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 minutes. The inhibitory constant (Ki) against FXa is calculated according to the Cheng–Prusoff equation. The IC50 is the amount of inhibitor required to diminish the initial velocity of the control by 50%.
Cell Research:

[2]

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  • Cell lines: Caco-2, wild-type, and P-gp-overexpressing LLC-PK1
  • Concentrations: 0 - 100 μM
  • Incubation Time: 2 hours
  • Method:

    LLC-PK1 and L-MDR1 cells are seeded in 96-well culture plates with microporous polycarbonate inserts and grown for 4 days in the same medium as used for cell cultures but without vincristine. The medium is replaced every 2 days. Before running the assay, the culture medium is replaced by HBSS buffer supplemented with 10 mM HEPES. Rivaroxaban are dissolved in DMSO and diluted with transport buffer to the respective final test concentrations (final DMSO concentration is always 1%). For inhibitor studies, the inhibitor is added at the appropriate concentration. counted. After 2 hour incubation at 37 °C, samples are taken from both compartments and, after the addition of ammonium acetate buffer and acetonitrile, are analyzed by LC-MS/M


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Fasted, male Wistar rats (HsdCpb:WU) and fasted, female New Zealand White rabbits (Esd:NZW).
  • Formulation: Rivaroxaban dissolves in polyethylene glycol/H2O/ glycerol (996 g/100 g/60 g) and is given by i.v. Rivaroxaban dissolved in solutol/ethanol/H2O [40%/10%/50% (v/v/v)] and is given by p.o.
  • Dosages: ≤0.3 mg/kg for i.v. and ≤3 mg/kg for p.o.
  • Administration: Administered via i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (199.59 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose+0.2% Tween 80 5 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 435.88
Formula

C19H18ClN3O5S

CAS No. 366789-02-8
Storage powder
in solvent
Synonyms BAY 59-7939

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01720108 Active, not recruiting Venous Thromboembolism David Anderson|Canadian Institutes of Health Research (CIHR)|Nova Scotia Health Authority February 24, 2013 Phase 3
NCT02970773 Not yet recruiting Spinal Cord Injuries|Thromboembolism Swiss Paraplegic Centre Nottwil January 2017 --
NCT02744092 Recruiting Cancer|Venous Thromboembolism|Deep Vein Thrombosis (DVT)|Pulmonary Embolism (PE)|Blood Clot Alliance Foundation Trials, LLC.|Patient-Centered Outcomes Research Institute December 2016 --
NCT02832531 Not yet recruiting Rheumatic Heart Disease Population Health Research Institute|University of Cape Town December 2016 Phase 3
NCT02975453 Recruiting Atrial Fibrillation Bayer|Janssen Research & Development, LLC December 2016 --
NCT02996435 Recruiting Atrial Fibrillation Janssen Scientific Affairs, LLC December 2016 Phase 4

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Factor Xa Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID