Apixaban

SKU: orb1307573

Description

Apixaban

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 503612-47-3
• MW: 459.5
• Purity: >98%
• Formula: C₂₅H₂₅N₅O₄
• SMILES: O=C1C=2N(N=C(C(N)=O)C2CCN1C3=CC=C(C=C3)N4C(=O)CCCC4)C5=CC=C(OC)C=C5
• Target: Protease
• Solubility: Soluble in DMSO (40 mg/ml)

Bioactivity

• Target IC50:
  FXa (rabbit):0.17 nM(Ki)|FXa (human):0.08 nM(Ki)
• In Vivo:
  When applied to normal human plasma in vitro, Apixaban extends coagulation time, doubling the prothrombin time (3.6 μM), modified prothrombin time (0.37 μM), activated partial thromboplastin time (7.4 μM), and HepTest (0.4 μM). Apixaban exhibits high selectivity in inhibiting human and rabbit Factor Xa, with Ki values of 0.08 and 0.17 nM, respectively. Additionally, Apixaban demonstrates maximum effectiveness in human and rabbit plasma in PT (Prothrombin Time) and APTT (Activated Partial Thromboplastin Time) assays, with comparatively lesser effects observed in rat and dog plasma.
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• In Vitro:
  Apixaban demonstrates excellent pharmacokinetic properties in dogs, characterized by very low clearance (Cl: 0.02 L/kg/h), low volume of distribution (Vdss: 0.2 L/kg), a half-life (T1/2: 5.8 h), and oral bioavailability (F: 58%). Its antithrombotic efficacy is evident in models of venous thrombosis, arteriovenous shunt thrombosis, and electrically induced carotid artery thrombosis in rabbits, with EC50 values of 110 nM, 270 nM, and 70 nM, respectively.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS-562247-01

Compound Identifiers

PubChem CID

10182969