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.
|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).
|Incubation time||3 min|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥18 mg/mL|
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.
Carter et al. J Thromb Thrombolysis. 2012 Aug 4. PMID: 22865256.
Safety and efficacy of apixaban in the treatment of atrial fibrillation.
Martin et al. Clin Med Insights Cardiol. 2012;6:103-9. PMID: 22844196.
Apixaban: a new player in the anticoagulant class.
Agrawal et al. Curr Drug Targets. 2012 Jun;13(6):863-75. PMID: 22250655.
Apixaban in patients with atrial fibrillation.
Connolly et al. N Engl J Med. 2011 Mar 3;364(9):806-17. PMID: 21309657.
Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies.
Wong PC, et al. J Thromb Haemost. 2008 May;6(5):820-9. PMID: 18315548.
|Related Factor Xa Products|
Ozagrel(OKY-046) sodium salt is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM.
Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant compound.
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.