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Apixaban

SKU: orb1307573

Description

Apixaban

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number503612-47-3
MW459.5
Purity>98%
FormulaC25H25N5O4
SMILESO=C1C=2N(N=C(C(N)=O)C2CCN1C3=CC=C(C=C3)N4C(=O)CCCC4)C5=CC=C(OC)C=C5
TargetProtease
SolubilitySoluble 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.
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.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

BMS-562247-01

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Key Properties

No computed properties available.

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Apixaban (orb1307573)

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5 mg
¥ 2,210.00
25 mg
¥ 4,290.00
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