5-R-RivaroxabanFactor Xa (FXa) inhibitor CAS# 865479-71-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 865479-71-6 | SDF | Download SDF |
PubChem ID | 11524901 | Appearance | Powder |
Formula | C19H18ClN3O5S | M.Wt | 435.88 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | BAY 59-7939 | ||
Solubility | DMSO : 33.33 mg/mL (76.47 mM; Need ultrasonic) | ||
Chemical Name | 5-chloro-N-[[(5R)-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-CQSZACIVSA-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)/t14-/m1/s1 | ||
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. |
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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. |
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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. |
Description | 5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) 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: |
5-R-Rivaroxaban Dilution Calculator
5-R-Rivaroxaban Molarity Calculator
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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5-R-Rivaroxaban is a selective inhibitor of human Factor Xa with IC50 value of 0.7 nmol/L [1].
Factor Xa is a serine endopeptidase enzyme and plays an important role in the convergence point of the intrinsic and extrinsic pathways in blood coagulation system [2].
5-R-Rivaroxaban is an oral, direct factor Xa inhibitor and the inhibition is species-dependent. When tested with purified factoe Xa from human or rabbit, 5-R-Rivaroxaban showed similar affinity with IC50 value of 0.7 nmol/L and 0.8 nmol/L, respectively, while had a IC50 value as low as 3.4 nmol/L when tested with rat factor Xa [1].
Pre-treated anaesthetised rat model with intravenous 5-R-Rivaroxaban at a dose of 2 mg/kg, and after bleeding initiated intravenous treated with rFVIIa (100/400 μg/kg), PCC (25/50 U/kg) or aPCC (50/100 U/kg), the result showed that 5-R-Rivaroxaban pre-treatment significantly shorten bleeding time and clotting time compared with 5-R-Rivaroxaban alone treated group [2]. Similar results were obtained when tested with rabbit model [1].
It has been reported that 5-R-Rivaroxaban is a promising drug for atrial fibrillation, venous thromboembolism or thromboembolic disorders in clinic [3] [4] [1].
References:
[1]. Perzborn, E., et al., Rivaroxaban: a new oral factor Xa inhibitor. Arterioscler Thromb Vasc Biol, 2010. 30(3): p. 376-81.
[2]. Perzborn, E., et al., Reversal of rivaroxaban anticoagulation by haemostatic agents in rats and primates. Thromb Haemost, 2013. 110(1): p. 162-72.
[3]. Beyer-Westendorf, J., et al., Efficacy and safety of rivaroxaban or fondaparinux thromboprophylaxis in major orthopedic surgery: findings from the ORTHO-TEP registry. J Thromb Haemost, 2012. 10(10): p. 2045-52.
[4]. Palareti, G., et al., Clinical management of rivaroxaban-treated patients. Expert Opin Pharmacother, 2013. 14(5): p. 655-67.
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