Rivaroxaban (C007B-253844)

Rivaroxaban is an oral, direct inhibitor of Factor X, being developed for the prevention and treatment of arterial and venous thrombosis with a Ki of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity (IC50 = 2.1 nM). Rivaroxaban also shows a similar affinity to purified human (IC50 = 0.7 nM) and rabbit Factor X (IC50 = 0.8 nM), but a lesser potency against purified rat Factor X (IC50 = 3.4 nM). Endogenous human and rabbit Factor X 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.

Specifications and Purity: ≥99%

Molecular Formula: C19H18ClN3O5S

Molecular Weight: 435.88

EC Number: 685-132-2

PubChem CID: 9875401

Isomeric SMILES: C1COCC(=O)N1C2=CC=C(C=C2)N3C[C@@H](OC3=O)CNC(=O)C4=CC=C(S4)Cl

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