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Apixaban

Cat. No. M1649
Apixaban Structure
Synonym:

BMS-562247-01

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 40  USD40 In stock
5mg USD 35  USD35 In stock
10mg USD 50  USD50 In stock
50mg USD 90  USD90 In stock
100mg USD 115  USD115 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Apixaban is a direct Human Factor Xa inhibitor with Ki of 0.08 nM. Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM and 0.4 μM in vitro. Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo.

Protocol
Cell Experiment
Cell lines
Preparation method Platelet aggregation assays
Platelet aggregation was measured in citrated human and rabbit platelet-rich plasma (PRP) in vitro with a platelet aggregometer (Model PAP-4D, BioData, Horsham, PA, USA). PRP was obtained from citrated blood after centrifuging at 250 · g for 6 min. Citrated PRP (250 μL) was mixed with 20 μL of vehicle, DMP802 at 3 μM or apixaban at 1–10 μM, and incubated for 3 min at 37℃. DMP802, a glycoprotein (GP)IIb/IIIa receptor antagonist, was included as a positive control (IC50 = 29 nM against human platelet aggregation response to 10 μM ADP). Peak platelet aggregation was determined after the addition of 20 μL of the agonist (ADP at 10 μM, c-thrombin at 35 nM, and collagen at 10 μg mL)1, final concentration).
Concentrations 1-10 μM
Incubation time 3 min
Animal Experiment
Animal models rat AVST model
Formulation 10% N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water
Dosages 0.03, 0.1, 0.3, 1mg/kg/h
Administration intravenously
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 459.5
Formula C25H25N5O4
CAS Number 503612-47-3
Purity >99%
Solubility DMSO 16 mg/mL
Storage at -20°C
References

[1] Carter et al. J Thromb Thrombolysis. Analysis of the projected utility of dabigatran, rivaroxaban, and apixaban and their future impact on existing Hematology and Cardiology Anticoagulation Clinics at The Johns Hopkins Hospital.

[2] Martin et al. Clin Med Insights Cardiol. Safety and efficacy of apixaban in the treatment of atrial fibrillation.

[3] Agrawal et al. Curr Drug Targets. Apixaban: a new player in the anticoagulant class.

[4] Connolly et al. N Engl J Med. Apixaban in patients with atrial fibrillation.

[5] Wong PC, et al. J Thromb Haemost. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Apixaban, BMS-562247-01 supplier, Factor Xa, inhibitors

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