What is Rivaroxaban?
Rivaroxaban is a new oral anticoagulant drug, a selective FXa inhibitor that acts on the active site of factor Xa (FXa). It inhibits FXa and inhibits the intrinsic and extrinsic coagulation pathways in a dose-dependent manner to inhibit thrombosis. It can be used for adult patients undergoing elective hip or knee replacement surgery to prevent venous thrombosis, and can also be used for adult patients with non-valvular atrial fibrillation with a history of stroke or transient ischemic attack to reduce the risk of stroke and systemic embolism.
Rivaroxaban powder is a white to off-white powder, insoluble in water; insoluble in ethanol; ≥13.9 mg/mL in DMSO under mild heating
| Product name | Rivaroxaban |
| CAS | 366789-02-8 |
| Molecular formula | C19H18ClN3O5S |
| Molecular weight | 435.88 |
| EINECS Number | 685-132-2 |
| Storage condition | Inert atmosphere,2-8°C |
| Melting point | 228-229°C |
| Solubility | Insoluble in water; Insoluble in ethanol; ≥13.9 mg/mL in DMSO under mild heating. |
| Appearance | White to off-white powder |
| Boiling point | 732.6±60.0 °C(Predicted) |
| Density | 1.460±0.06 g/cm3(Predicted) |
What is the mechanism of Rivaroxaban?
Rivaroxaban inhibits free and bound coagulation factor Xa in prothrombinase complex. It is a selective direct coagulation factor Xa inhibitor, and its onset time is 2.5 to 4 hours. The inhibition of coagulation factor Xa will interrupt the internal and external pathways of coagulation cascade, thus inhibiting the formation of thrombin and the development of thrombus. Rivaroxaban does not inhibit thrombin (activated coagulation factor II) and has been shown to have no effect on platelets.
Product Specification
| Item | Specification | Results |
| Appearance | White powder | Complies |
| ldentification | IR:similar to Reference Standard | Complies |
| Appearance of solution | Clear and colorless | Complies |
| Loss on Drying | ≤0.5% | 0.06% |
| Sulphated Ash | ≤0.2% | 0.03% |
| Heavy metals | ≤0.002% | Complies |
| Related Compounds | Single Impurity ≤1.0% | Complies |
| Sum of Impurity≤2.0% | Complies | |
| Assay | 98.0%to 101.5% | 99.80% |
| Conclusion: | Conform with enterprise specification. |
What are the applications of rivaroxaban?
1. Rivaroxaban powder is used for people who are undergoing elective hip or knee replacement surgery to prevent venous thrombosis (VTE).
2. It is used for adult venous thrombosis (DVT) to reduce the risk of DVT recurrence and pulmonary embolism (PE) after acute DVT.
3. It is used for adult patients with non-valvular atrial fibrillation with one or more risk factors to reduce the risk of stroke and systemic embolism.
4. The essential difference between rivaroxaban and fondaparinux sodium/heparin is that it does not require the participation of antithrombin III, but can directly antagonize free and bound Xa factors to reduce the activation of thrombin and thus prolong the coagulation time. It not only has a blocking effect on the formation of blood clots, but also can destroy the formed blood clots.
HTML5 atlas of Rivaroxaban
|
|
Biological Activity of Rivaroxaban
| Description | Rivaroxaban is a highly potent and selective Factor Xa (FXa) inhibitor with potent anti-FXa activity (IC50 of 0.7 nM, Ki of 0.4 nM). |
| In vitro studies | Rivaroxaban (BAY 59-7939) is an oral, direct factor Xa (FXa) inhibitor used for the prevention and treatment of arterial and venous thrombosis. Rivaroxaban competitively inhibits human FXa (Ki 0.4 nM) with 10 000-fold selectivity over 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 in rat plasma (IC50 290 nM). It shows an anticoagulant effect in human plasma, doubling the prothrombin time (PT) and activating the partial thromboplastin time at 0.23 and 0.69 μM, respectively. |
| In vivo studies | Rivaroxaban (BAY 59-7939) is a potent, selective, direct FXa inhibitor with excellent in vivo activity and good oral bioavailability. Rivaroxaban (BAY 59-7939), given by intravenous bolus before thrombus induction, reduced thrombus formation (ED50 0.1 mg/kg), inhibited FXa, and prolonged PT in a dose-dependent manner. PT50 and FXa were slightly affected at ED50 (1.8-fold increase and 32% inhibition, respectively). At 0.3 mg/kg (a dose that almost completely inhibited thrombus formation), rivaroxaban modestly prolonged PT (3.2±0.5-fold) and inhibited FXa activity (65±3%). |
| Kinase assay | The activity of rivaroxaban (BAY 59-7939) against purified serine proteases was measured using chromogenic or fluorogenic substrates in 96-well microtiter plates at 25°C. The enzyme was incubated with rivaroxaban or its solvent DMSO for 10 minutes. The reaction was initiated by the addition of substrate and the color or fluorescence was monitored continuously at 405 nm using a Spectra Rainbow Thermo Reader or at 630/465 nm using a SPECTRAfluor plus, respectively, for 20 minutes. Enzyme activity was analyzed in the following buffers (final concentration): 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 chromothiocyanate 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; chromothiocyanate TH (200 μM), chromothiocyanate plasmin (500 μM), or chromothiocyanate inhibitor (500 μM), FXIa (1 nM), or APC (10 nM) in 50 mM phosphate buffer, pH 7.4, 150 mM NaCl; and S 2366 (150 or 500 μM) 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, HD-Phe-Pro-Arg-6-amino-1-naphthalene-benzylsulfonamide in H2O (100 μM) and measured for 3 hours. FIXab/FX assay, including 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, was started by adding I-1100 (50 μM) and measured for 60 minutes. The inhibition constant (Ki) against FXa was 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 was determined from the Lineweaver-Burk plot. IC50 is the inhibitory dose required to reduce the initial velocity of the control by 50%. |
| Animal experiments | Rats[2] Fasted male Wistar rats (HsdCpb:WU) were used. The rat venous stasis model induced thrombosis in anesthetized rats (n = 10 per dose group) with minor modifications. The abdominal vena cava was exposed and two loose sutures (8–10 mm apart) were placed below the branches of the left renal vein. Ribaxaban was dissolved in polyethylene glycol/H2O/glycerol (996 g/100 g/60 g) or vehicle was administered by intravenous (iv) bolus injection into the tail vein 15 minutes before thrombus induction. Thromboplastin (0.5 mg/kg) was injected into the femoral vein and 15 seconds later, the proximal and distal sutures were tied. After 15 minutes, the ligated segment was removed and the thrombus was aspirated and weighed. Blood samples were 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. |
What is the difference between rivaroxaban and aspirin?
The differences between rivaroxaban and aspirin are different in action mechanism, efficacy and contraindications.
1. Different action mechanism: rivaroxaban powder has a highly selective inhibitory effect on coagulation factor X, inhibiting the function of coagulation factor X in exogenous or endogenous coagulation cascade reactions, thereby achieving anticoagulant effect; aspirin is a non-selective COX-2 (cyclooxygenase 2) inhibitor, which inhibits platelet aggregation by inhibiting the production of prostaglandins.
2. Different efficacy: rivaroxaban is mainly used to prevent venous thrombosis, reduce the risk of pulmonary embolism, and reduce the risk of thrombosis in patients with myocardial infarction and atrial fibrillation after hip or knee replacement surgery; aspirin is mainly used to treat inflammatory diseases such as rheumatoid arthritis and osteoarthritis and prevent arterial thrombosis in patients with myocardial infarction.
3. Different contraindications: rivaroxaban is contraindicated in patients with active internal bleeding, severe liver dysfunction, pregnant and lactating patients, and those who are allergic to the drug; aspirin is contraindicated in patients with active internal bleeding and those who are allergic to the drug.
What are the contraindications for using Rivaroxaban powder?
1 Patients who are allergic to any excipients of rivaroxaban powder.
2 Patients with clinically apparent active bleeding.
3. Lesions or conditions with significant risk of major bleeding.
4 Patients with liver disease with coagulation abnormalities and clinically relevant bleeding risks, including patients with cirrhosis up to Child Pugh classes B and C.
How and where to buy Rivaroxaban Powder wholesale?
You can trust our order because we have a good record of selling legal educational drugs.
We conduct independent laboratory tests on all products and then sell them to our respected customers.
Send your Inquiry for more details, Click email：allen@faithfulbio.com Now.
A variety of shipping methods for you to choose
|
Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
DHL, Germany DHL, Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
|
7-15 days |
By Air |
Suitable for more than 50kg. |
|
|
15-60 days |
By Sea |
Suitable for more than 500kg. |
Send your Inquiry for more details, Click email：allen@faithfulbio.com Now.
Disclaimer: The articles published on this site are mainly used to promote academic exchanges and learning, and do not mean that this site agrees with its views or confirms the authenticity of its contents. Please filter carefully. If you believe this article is infringing, please contact the administrator. We are not responsible for the consequences of using the information and services on this website.
Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
Hot Tags: rivaroxaban powder cas 366789-02-8, China, suppliers, manufacturers, factory, customized, wholesale, buy, price, bulk, pure, producer, discount, for sale, in stock, free sample, raw powder, raw material, made in China