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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. In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produces dose-dependent antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM, respectively.
| 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 |
| Molecular Weight | 459.5 |
| Formula | C25H25N5O4 |
| CAS Number | 503612-47-3 |
| Solubility (25°C) | DMSO 46 mg/mL |
| Storage | Powder -20°C |
[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.
| Related Factor Xa Products |
|---|
| Darexaban
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. |
| Eribaxaban
Eribaxaban (PD-0348292) is an orally active and selective FXa inhibitor with a Ki value of 0.32 nM. |
| Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride
Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride is a factor Xa specific chromogenic substrate. |
| D-Pro-Phe-Arg-Chloromethylketone
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation. |
| Methoxycarbonyl-D-Nle-Gly-Arg-pNA
Methoxycarbonyl-D-Nle-Gly-Arg-pNA is a synthetic trypsin that can serve as a substrate for coagulation factors IXa (FIXa) and Xa (FXa). |
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