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Apixaban
| Product Name | Apixaban |
| Price: | Inquiry |
| Catalog No.: | CN00214 |
| CAS No.: | 503612-47-3 |
| Molecular Formula: | C25H25N5O4 |
| Molecular Weight: | 459.5 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | COc1ccc(cc1)n1nc(c2c1C(=O)N(CC2)c1ccc(cc1)N1CCCCC1=O)C(=O)N |
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| Description | Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. |
| Target | IC50: 0.08 nM (Human Factor Xa), 0.17 nM (Rabbit Factor Xa) |
| In Vitro | Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively[1]. In vitro, 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, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays[2]. |
| In Vivo | Apixaban shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L/kg/h), and low volume of distribution (Vdss: 0.2 L/kg) in the dogs. Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%)[1]. 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[2]. Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo[3]. In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L/kg), low systemic clearance (Cl: 0.018 L/kg/h), and good oral bioavailability (F: 59%)[4]. |
| Animal Admin | Briefly, male New Zealand White rabbits are anesthetized with ketamine (50 mg/kg i.m.) and xylazine (10 mg/kg i.m.), and their femoral artery, jugular vein and femoral vein are catheterized. These anesthetics are supplemented as needed. Thrombosis is induced by an arteriovenous (AV)-shunt device containing a silk thread. Blood flowed from the femoral artery via the AV shunt into the opposite femoral vein for 40 min. The shunt is then disconnected and the silk thread covered with thrombus is weighed. As apixaban has an oral bioavailability of < 5% in rabbits (unpublished result), it is administered intravenously for in vivo studies. To achieve a stable plasma level with minimum experimental variability, apixaban, fondaparinux or vehicle is given by a continuous intravenous infusion 1 h prior to shunt placement. The infusion is continued throughout the experiment. Warfarin or vehicle is dosed orally once daily for 4 days. On the fourth day after the last oral dose of warfarin or vehicle, rabbits are anesthetized 1.5 h later, and the treatment effect is evaluated about 2 h postdose. Arterial blood samples for the determination of clotting times or plasma levels are collected 20 min after shunt placement. Plasma levels of apixaban are measured by a specific and sensitive liquid chromatographic mass spectrometry method (LC/MS/MS). In rabbits treated with apixaban, fondaparinux or warfarin, the antithrombotic effects of these agents are expressed as percentage inhibition of thrombus formation based on the treated vs. the corresponding mean vehicle. The ED50 value (dose that produced 50% inhibition of thrombus formation) is determined as described below. The apixaban group treatment consists of vehicle (10%N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water) (n=4), and apixaban (mg/kg/h) at 0.03 (n=7), 0.1 (n=7), 0.3 (n=7), 1 (n=7), and 3 (n=3). The fondaparinux group treatment consists of vehicle (saline) (n=6), and fondaparinux (mg/kg/h1) at 0.01 (n=5), 0.03 (n=5), 0.1 (n=5), 0.3 (n=5), and 1 (n=5). The warfarin group treatment consists of vehicle (water) (n=6), and warfarin (mg/kg/day) at 0.1 (n=6), 0.3 (n=6), 1 (n=6), and 3 (n=6). |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 770.5±60.0 °C at 760 mmHg |
| Flash Point | 419.8±32.9 °C |
| Exact Mass | 459.190643 |
| PSA | 110.76000 |
| LogP | 0.48 |
| Vapour Pressure | 0.0±2.6 mmHg at 25°C |