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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.
| 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 |
| 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.
| Molecular Weight | 459.5 |
| Formula | C25H25N5O4 |
| CAS Number | 503612-47-3 |
| Purity | >99% |
| Solubility | DMSO 16 mg/mL |
| Storage | at -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 |
|---|
| Ozagrel sodium
Ozagrel(OKY-046) sodium salt is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. |
| Ozagrel
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. |
| Edoxaban Tosylate Monohydrate
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
Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a). |
| Rivaroxaban
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. |
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