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Rivaroxaban

Factor Xa inhibitor CAS# 366789-02-8

Rivaroxaban

2D Structure

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Rivaroxaban

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Chemical Properties of Rivaroxaban

Cas No. 366789-02-8 SDF Download SDF
PubChem ID 6433119 Appearance Powder
Formula C19H18ClN3O5S M.Wt 435.88
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BAY 59-7939
Solubility Soluble in DMSO > 10 mM
Chemical Name 5-chloro-N-[[2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide
SMILES C1COCC(=O)N1C2=CC=C(C=C2)N3CC(OC3=O)CNC(=O)C4=CC=C(S4)Cl
Standard InChIKey KGFYHTZWPPHNLQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H18ClN3O5S/c20-16-6-5-15(29-16)18(25)21-9-14-10-23(19(26)28-14)13-3-1-12(2-4-13)22-7-8-27-11-17(22)24/h1-6,14H,7-11H2,(H,21,25)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Rivaroxaban

DescriptionRivaroxaban is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).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 (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].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].

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) [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.

Protocol

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 (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].

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.

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) [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.

Rivaroxaban Dilution Calculator

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Preparing Stock Solutions of Rivaroxaban

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2942 mL 11.471 mL 22.9421 mL 45.8842 mL 57.3552 mL
5 mM 0.4588 mL 2.2942 mL 4.5884 mL 9.1768 mL 11.471 mL
10 mM 0.2294 mL 1.1471 mL 2.2942 mL 4.5884 mL 5.7355 mL
50 mM 0.0459 mL 0.2294 mL 0.4588 mL 0.9177 mL 1.1471 mL
100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.4588 mL 0.5736 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Rivaroxaban

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2-carboxamide, is a potent small-molecule inhibitor of factor Xa which is a coagulation factor at a critical juncture in the blood coagulation pathway resulting in the generation of thrombin and the formation of clot. Rivaroxaban binds to the Tyr288 in S1 pocket of factor Xa through the interaction of Tyr288 and the chlorine substituent of the chlorothiophene moiety. The inhibition is reversible (koff = 5x10-3s-1), rapid (kon = 1.7x107 mol/L-1 s-1), and in a concentration-dependent manner (Ki = 0.4 nmol/L). Rivaroxaban is currently being studied for the treatment of VTE, prevention of cardiovascular events in patients with acute coronary syndrome, prevention of stroke in patients with atrial fibrillation.

Reference

Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, and Volker Laux. Rivaroxaban: a new oral factor Xa inhibitor. Arterioscler Thromb Vasc Biol 2010; 30(3): 376-381

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References on Rivaroxaban

Importance of balancing follow-up time and impact of oral-anticoagulant users' selection when evaluating medication adherence in atrial fibrillation patients treated with rivaroxaban and apixaban.[Pubmed:28366075]

Curr Med Res Opin. 2017 Jun;33(6):1033-1043.

OBJECTIVE: Studies comparing medications adherence have become common yet they often do not account for differences in relative follow-up. Patient selection criteria may impact validity and comparability of these studies as well. METHODS: Adults with non-valvular atrial fibrillation, >/=1 Rivaroxaban or apixaban dispensing (index date), and >/=1 year of pre-index eligibility were selected from IMS Health Real World Data Adjudicated Claims (IMS RWD Adjudicated Claims) and Truven Health MarketScan Research (Truven MarketScan) databases. Adherence was evaluated using proportion of days covered (PDC) >/= 0.8 for treatment cohorts: (1) unmatched, with different follow-up, (2) propensity-score matched with similar follow-up, (3) matched, with similar follow-up and >/=2 Rivaroxaban or apixaban dispensings, and (4) matched, with similar follow-up and chronic medication users only. Robustness was verified with PDC >/=0.9. RESULTS: In the IMS RWD Adjudicated Claims database, Rivaroxaban users had a longer mean follow-up than apixaban users (408 versus 254 days, respectively; p < .01). While crude comparisons demonstrated lower adherence rates for Rivaroxaban than apixaban (-12.4 percentage points [pp]; p < .05), these difference attenuated after matching and (1) balancing follow-up (-2.2 pp; p < .05), (2) excluding single-time medication users (0.2 pp; p > .05), and reversed after (3) excluding non-chronic medication users (5.0 pp; p < .05). Results obtained were consistent when these analyses were repeated within the Truven MarketScan databases and when using a PDC >/=0.9. CONCLUSION: Medication adherence comparisons need to account for differences in follow-up. Selection of chronic medication users may impact comparative adherence advantage between medications.

Treatment application of rivaroxaban in Chinese patients with livedoid vasculopathy.[Pubmed:28360530]

J Pain Res. 2017 Mar 17;10:621-624.

Livedoid vasculopathy (LV) is a chronic prothrombotic disease of cutaneous micro-circulation resulting in cutaneous ischemia and infarction. As a rare disease, LV has an estimated incidence of ten cases per million. Not only correct diagnosis but also effective treatments are very difficult for patients with LV. Due to the lack of large-scale studies in this rare disease, LV poses a great challenge to the doctors, and existing treatment has always been an individual attempt with off-label application. The main goals in the treatment of patients with LV are to avoid the repeated occurrence of active cutaneous lesions and prevent painful ulceration and irreversible scarring. The current report describes the cases of three Chinese patients with LV receiving Rivaroxaban treatment, an oral direct inhibitor of factor Xa inhibitor, and observes the treatment effect of Rivaroxaban during the follow-up. As an injection-free alternative to low-molecular-weight heparin (LMWP) and monitoring-free alternative to warfarin, Rivaroxaban improves the quality of life and enhances the compliance of patients. All patients consider Rivaroxaban as more tolerable than previous drugs and, therefore, continue the application of Rivaroxaban, effectively improving the treatment effect of drugs and successfully avoiding the repeated occurrence of active cutaneous lesions. Treatment application of Rivaroxaban in Chinese patients with LV successfully avoids the recurrence of active cutaneous lesions and prevents the progressive ulceration and scarring.

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).

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