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Purity: ≥98%
Rivaroxaban (BAY59-7939; BAY-59-7939; trade name: Xarelto), an approved anticoagulant drug used to treat and prevent blood clots, is the first orally bioavailable, selective and direct inhibitor of Factor Xa with potential anti-coagulant activity. It inhibits Factor Xa with a Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively. Rivaroxaban binds to the Tyr288 in S1 pocket of factor Xa through the interaction of Tyr288 and the chlorine substituent of the chlorothiophene moiety. Rivaroxabanis used as an oral anticoagulant developed by Bayer amd was marketed in many countries with the trade name of Xarelto. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs four hours after a dose. The effects lasts 8–12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible.
| ln Vitro |
An oral direct Factor Xa (FXa) inhibitor called rivaroxaban (BAY 59-7939) is being developed for the treatment and prevention of venous and arterial thrombosis. Rivaroxaban inhibits prothrombinase activity (IC50 2.1 nM) and human FXa (Ki 0.4 nM) competitively with selectivity that is >10,000 times better than that of other serine proteases. In comparison to rat plasma (IC50 290 nM), human and rabbit plasma exhibit a more effective inhibition of endogenous FXa by rivaroxaban (IC50 21 nM). In human plasma, it exhibits anticoagulant properties, activating partial thromboplastin time at 0.69 μM and increasing prothrombin time (PT)[2].
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| ln Vivo |
A strong and specific direct FXa inhibitor with good oral absorption and in vivo action is rivaroxaban (BAY 59-7939)[1]. When given as an intravenous bolus prior to thrombus induction, rivaroxaban (BAY 59-7939) decreases thrombus formation (ED50 0.1 mg/kg), suppresses FXa, and dose-dependently prolongs PT. At the ED50, there is a small change in PT and FXa (1.8-fold increase and 32% inhibition, respectively). At a dosage of 0.3 mg/kg, which virtually completely blocks thrombus formation, rivaroxaban exhibits a moderate prolongation of PT (3.2±0.5-fold) and a suppression of FXa activity (65±3%)[2].
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| 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 |
| Molecular Formula |
C19H18CLN3O5S
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|---|---|
| Molecular Weight |
435.88
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| CAS # |
366789-02-8
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| Related CAS # |
Rivaroxaban-d4;1132681-38-9
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| SMILES |
O=C(C1=CC=C(Cl)S1)NC[C@H]2CN(C3=CC=C(N4C(COCC4)=O)C=C3)C(O2)=O
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| Synonyms |
BAY 59-7939; Rivaroxaban; BAY59-7939; BAY-59-7939; trade name: Xarelto.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2942 mL | 11.4710 mL | 22.9421 mL | |
| 5 mM | 0.4588 mL | 2.2942 mL | 4.5884 mL | |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2942 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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