Rivaroxaban

SKU: orb1309486

Description

Rivaroxaban

Research Area

Metabolism Research

Key Properties

• CAS Number: 366789-02-8
• MW: 435.88
• Purity: 99.96%
• Formula: C₁₉H₁₈ClN₃O₅S
• SMILES: O=C1N(C[C@H](CNC(=O)C=2SC(Cl)=CC2)O1)C3=CC=C(C=C3)N4C(=O)COCC4
• Target: Factor Xa
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (7.57 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:82.5 mg/mL (189.27 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  FXa:0.7 nM|Prothrombinase:2.1 nM
• In Vivo:
  Rivaroxaban is a direct inhibitor of activated Factor X (Ki: 0.4 nM) with an oral bioavailability profile and also exhibits inhibitory activity against prothrombinase (IC50: 2.1 nM), used in the prevention and treatment of venous and arterial thrombosis. It demonstrates a similar affinity for purified human and rabbit FXa (IC50: 0.7 nM and 0.8 nM, respectively) but a weaker affinity for rat FXa (IC50: 3.4 nM). In plasma, Rivaroxaban inhibits endogenous FXa in human and rabbit equivalently (IC50: 21 nM), whereas it is less effective in rat plasma (IC50: 290 nM). Rivaroxaban is identified as a P-glycoprotein (P-gp) substrate with polarized transport characteristics and high permeability in Caco-2 cells, and does not impact P-gp-mediated drug transport even at the concentration of 100 μM in in vitro experiments.
• In Vitro:
  In rat and rabbit arteriovenous shunt models, oral administration of Rivaroxaban significantly reduced arterial thrombus formation (ED50: 5.0 mg/kg and 0.6 mg/kg, respectively). Intravenous administration of Rivaroxaban in a rat venous stasis model showed a dose-dependent reduction in venous thrombus formation (ED50: 0.1 mg/kg). Within the study dosage range of 0.3-3 mg/kg for dogs and 1-10 mg/kg for rats, Rivaroxaban displayed linear pharmacokinetics. The compound was characterized by a low plasma clearance rate in both species (dogs: 0.3 L/(kg·h), rats: 0.4 L/(kg·h)) and a stable volume of distribution (V(ss)) (dogs: 0.4 L/kg, rats: 0.3 L/kg). Rivaroxaban also had a short elimination half-life following oral administration in both species (0.9-2.3 h).
• Cell Research:
  LLC-PK1 and L-MDR1 cells are seeded in 96-well culture plates with microporous polycarbonate inserts and grown for 4 days in the same medium as used for cell cultures but without vincristine. The medium is replaced every 2 days. Before running the assay, the culture medium is replaced by HBSS buffer supplemented with 10 mM HEPES. Rivaroxaban are dissolved in DMSO and diluted with transport buffer to the respective final test concentrations (final DMSO concentration is always 1%). For inhibitor studies, the inhibitor is added at the appropriate concentration. counted. After 2 hour incubation at 37 °C, samples are taken from both compartments and, after the addition of ammonium acetate buffer and acetonitrile, are analyzed by LC-MS/M (Only for Reference)

Storage & Handling

• Storage: store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Fxa, Factor Xa, FactorXa, BAY 59-7939, Thrombin, Rivaroxaban

Compound Identifiers

PubChem CID

9875401