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5-R-Rivaroxaban

Catalog No. T10174   CAS 865479-71-6

5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor (IC50 0.7 nM; Ki 0.4 nM).

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5-R-Rivaroxaban Chemical Structure
5-R-Rivaroxaban, CAS 865479-71-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 55.00
25 mg In stock $ 122.00
50 mg In stock $ 228.00
100 mg In stock $ 393.00
200 mg In stock $ 582.00
500 mg In stock $ 913.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 98.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor (IC50 0.7 nM; Ki 0.4 nM).
Targets&IC50 FXa:0.7 nM
In vitro 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, 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].
Molecular Weight 435.88
Formula C19H18ClN3O5S
CAS No. 865479-71-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.33 mg/mL (76.47 mM), Sonification is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Coagulation and Anticoagulation Compound Library Metabolism Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library Bioactive Compound Library

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Keywords

5-R-Rivaroxaban 865479-71-6 Metabolism Factor Xa 5 R Rivaroxaban Fxa Inhibitor inhibit 5RRivaroxaban inhibitor

 

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