Rivaroxaban [366789-02-8]
Cat# HY-50903-50mg
Size : 50mg
Brand : MedChemExpress
Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
For research use only. We do not sell to patients.
Rivaroxaban Chemical Structure
CAS No. : 366789-02-8
Based on 14 publication(s) in Google Scholar
Other Forms of Rivaroxaban:
- Rivaroxaban-d4 In-stock
Description |
Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM)[1][2]. |
IC50 & Target |
IC50: 0.7 nM (FXa)[1]
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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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
435.88 |
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Formula |
C19H18ClN3O5S |
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CAS No. |
366789-02-8 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
O=C(N(C1=CC=C(N2C(COCC2)=O)C=C1)C3)O[C@H]3CNC(C4=CC=C(S4)Cl)=O |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 50 mg/mL (114.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Purity & Documentation |
Purity: 99.93% ee.: 99.97% |
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References |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.2942 mL | 11.4710 mL | 22.9421 mL | 57.3552 mL |
5 mM | 0.4588 mL | 2.2942 mL | 4.5884 mL | 11.4710 mL | |
10 mM | 0.2294 mL | 1.1471 mL | 2.2942 mL | 5.7355 mL | |
15 mM | 0.1529 mL | 0.7647 mL | 1.5295 mL | 3.8237 mL | |
20 mM | 0.1147 mL | 0.5736 mL | 1.1471 mL | 2.8678 mL | |
25 mM | 0.0918 mL | 0.4588 mL | 0.9177 mL | 2.2942 mL | |
30 mM | 0.0765 mL | 0.3824 mL | 0.7647 mL | 1.9118 mL | |
40 mM | 0.0574 mL | 0.2868 mL | 0.5736 mL | 1.4339 mL | |
50 mM | 0.0459 mL | 0.2294 mL | 0.4588 mL | 1.1471 mL | |
60 mM | 0.0382 mL | 0.1912 mL | 0.3824 mL | 0.9559 mL | |
80 mM | 0.0287 mL | 0.1434 mL | 0.2868 mL | 0.7169 mL | |
100 mM | 0.0229 mL | 0.1147 mL | 0.2294 mL | 0.5736 mL |
Rivaroxaban Related Classifications
- Metabolic Enzyme/Protease
- Factor Xa