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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.
| Related Factor Xa Products |
|---|
| Rivaroxaban
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. |
| Betrixaban
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a). |
| Edoxaban Tosylate Monohydrate
Edoxaban tosylate monohydrate is a selective factor Xa inhibitor with Ki of 0.561 nM, >10000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant compound. |
| BMS-740808
BMS-740808 is a highly potent, selective inhibitor of blood coagulation factor Xa (fXa) with Ki with 0.03 nM. |
| Ozagrel
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. |
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