Catalog No.S3002 Synonyms: BAY 59-7939
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).
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a, BMDMs were pretreated with or without 10 μM FXa inhibitor rivaroxaban or 10 μM DPP4 inhibitor KR62436, followed by incubation for 4 h with rFX or rDPP4 alone or in combination. Mcp1 mRNA was then quantified. n = 4 technical replicates per group; mean ± s.e.m.; *P < 0.05 by one-way ANOVA.
Nature, 2018, 555(7698):673-677. Rivaroxaban purchased from Selleck.
a) Correlation between rivaroxaban trough plasma concentrations measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and concentrations indirectly estimated by the rivaroxaban anti-FXa activity assay for all samples (15 and 20 mg OD, n = 71). The regression line is added.
Eur J Clin Pharmacol, 2016, 72(6):671-9 . Rivaroxaban purchased from Selleck.
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
|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).|
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).  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. 
|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.).  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). |
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%.
|In vitro||DMSO||87 mg/mL (199.59 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02864758||Recruiting||Atrial Fibrillation||Bayer|Janssen Scientific Affairs LLC||September 8 2016||--|
|NCT02401594||Terminated||Non-major Orthopaedic Surgery||Centre Hospitalier Universitaire de Saint Etienne|Bayer||December 8 2015||Phase 3|
|NCT03566303||Recruiting||Prostheses and Implants|Stroke|Valve Heart Disease|Anticoagulants and Bleeding Disorders||Hospital Geral Roberto Santos||June 6 2018||Phase 2|Phase 3|
|NCT03148457||Recruiting||Ischaemic Stroke||University Hospital Inselspital Berne||November 6 2017||Not Applicable|
|NCT03189069||Completed||Atrial Fibrillation||Bristol-Myers Squibb||October 6 2016||--|
|NCT02975453||Active not recruiting||Atrial Fibrillation||Bayer|Janssen Research & Development LLC||December 5 2016||--|
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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