For research use only.
Catalog No.S3002 Synonyms: BAY 59-7939
CAS No. 366789-02-8
Rivaroxaban (BAY 59-7939) 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).
Selleck's Rivaroxaban has been cited by 14 publications
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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.
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Choose Selective Factor Xa Inhibitors
|Description||Rivaroxaban (BAY 59-7939) 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04597593||Recruiting||--||Drug-Related Side Effects and Adverse Reactions|Iatrogenic Disorder||Cipherome Inc.|Seoul National University Bundang Hospital||October 7 2020||--|
|NCT03684564||Not yet recruiting||Drug: Rivaroxaban|Drug: Warfarin||Antiphospholipid Syndrome|Systemic Lupus Erythematosus|Stroke|Ischemic Stroke|Brain Ischemia||University College London|Arthritis Research UK|King''s College London|University College London Hospitals|Hammersmith Hospitals NHS Trust|Guy''s and St Thomas'' NHS Foundation Trust|Barts & The London NHS Trust|King''s College Hospital NHS Trust|Manchester University NHS Foundation Trust|Barking Havering and Redbridge University Hospitals NHS Trust|St George''s University Hospitals NHS Foundation Trust||September 2020||Phase 2|Phase 3|
|NCT04508439||Recruiting||Drug: Enoxaparin||Covid19|Pneumonia|Coagulation Disorder|Pulmonary Embolism||Hospital Regional de Alta especialidad de Ixtapaluca||June 20 2020||Not Applicable|
|NCT04356989||Recruiting||Drug: Rivaroxaban (Xarelto BAY59-7939)||Non-valvular Atrial Fibrillation (NVAF)||Bayer|Janssen Research & Development LLC||May 13 2020||--|
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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