[CAS NO. 366789-02-8] Rivaroxaban (BAY 59-7939)

Name: Rivaroxaban (BAY 59-7939)
Brand: Arctom Scientific
SKU: SLK-S3002

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PRODUCTS SPECIFICATIONS [366789-02-8]

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Catalog

SLK-S3002

Brand

Selleck

CAS

366789-02-8

DESCRIPTION [366789-02-8]

Overview

MDL	MFCD11974010
Molecular Weight	435.88
Molecular Formula	C19H18ClN3O5S
SMILES	O=C1N(C[C@H](CNC(=O)C=2SC(Cl)=CC2)O1)C3=CC=C(C=C3)N4C(=O)COCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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
50 mM	0.0459 mL	0.2294 mL	0.4588 mL

Description

Rivaroxaban (BAY 59-7939) is a direct inhibitor of with and of 0.4 nM and 0.7 nM in cell-free assays, respectively. It is selective for human factor Xa, for which it has >10 000-fold greater selectivity than for other biologically relevant serine proteases (IC50 >20 μM).

Targets

Factor Xa ^[1] (Cell-free assay)	Prothrombinase ^[1] (Cell-free assay)
0.7 nM	2.1 nM

In vitro

Rivaroxaban is an oral, direct inhibitor of Factor Xa (FXa), being developed for the prevention and treatment of arterial and venous thrombosis with a K of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity with IC50 of 2.1 nM. Rivaroxaban also shows a similar affinity to purified human and rabbit FXa (IC50 0.7 nM and 0.8 nM, respectively), but a lesser potency against purified rat FXa (IC50 3.4 nM). Endogenous human and rabbit FXa in plasma is inhibited to a similar extent by Rivaroxaban (IC50 21 nM and 21 nM, respectively), while 14-fold higher concentrations are required in rat plasma (IC50 290 nM). Rivaroxaban exhibits high permeability and polarized transport across Caco-2 cells as a substrate of the P-gp, but exhibits no inhibitory effect on P-gp-mediated drug transport up to concentrations of 100 μM in vitro.

In vivo

Rivaroxaban reduces venous thrombosis in a dose dependent manner (ED50 0.1 mg/kg i.v.) in a rat venous stasis model. Rivaroxaban reduces arterial thrombus formation in an arteriovenous (AV) shunt in rats (ED50 5.0 mg/kg p.o.) and rabbits (ED50 0.6 mg/kg p.o.). Plasma pharmacokinetics of Rivaroxaban are linear across the investigated dose range (1-10 mg/kg in rats, 0.3-3 mg/kg in dogs). Plasma clearance is low: 0.4 L/kg/h in rats and 0.3 L/kg/h in dogs; the volume of distribution (V(ss)) is moderate: 0.3 L/kg in rats, and 0.4 L/kg in dogs. The elimination half-life after oral administration is short in both species (0.9-2.3 hours).

References

[1] Perzborn E, et al. J Thromb Haemost, 2005, 3(3), 514–521.
[2] Gnoth MJ, et al. J Pharmacol Exp Ther, 2011, 338(1), 372-380.
[3] Weinz C, et al. Xenobiotica, 2005, 35(9), 891-910.

Synonyms

2-Thiophenecarboxamide, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-

5-Chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide

Rivaroxaban

BAY 59-7939

5-Chloro-N-[[(S)-3-(4-(3-oxomorpholin-4-yl)phenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]-thiophene-2-carboxamide

Xarelto

5-Chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl]methyl]-2-thiophenecarboxamide

5-Chloro-N-([(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl]-methyl)-2-thiophenecarboxamide

(S)-Rivaroxaban