5-R-Rivaroxaban

SKU: orb1310040

Description

5-R-Rivaroxaban

Research Area

Metabolism Research

Key Properties

• CAS Number: 865479-71-6
• MW: 435.88
• Purity: 99.75%
• Formula: C₁₉H₁₈ClN₃O₅S
• SMILES: ClC1=CC=C(S1)C(=O)NCC1CN(C(=O)O1)C1=CC=C(C=C1)N1CCOCC1=O
• Target: Factor Xa
• Solubility: DMSO:33.33 mg/mL (76.47 mM);10% DMSO+90% Corn Oil:2 mg/mL (4.59 mM)

Bioactivity

• Target IC50:
  FXa:0.7 nM
• 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%) .
• 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 .

Storage & Handling

• Storage: 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, Fxa, Factor Xa, FactorXa, Inhibitor, 5RRivaroxaban, 5-R-Rivaroxaban, 5 R Rivaroxaban

Compound Identifiers

PubChem CID

6433119