product name Apixaban
Description: Apixaban, also known as BMS-56224701, is a highly selective, reversible, direct inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is used as an anticoagulant for the treatment of venous thromboembolic events. Factor Xa is the activated form of the coagulation factorthrombokinase. Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants.
References: J Med Chem. 2007;50(22):5339-56; J Thromb Haemost. 2008;6(5):820-9; J Thromb Thrombolysis. 2010;29(1):70-80.
459.5
Formula
C25H25N5O4
CAS No.
503612-47-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 18 mg/mL (39.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
BMS 562247-01
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19420067
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In the dog, Apixaban shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1 h-1), and low volume of distribution (Vdss: 0.2 L kg-1). Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%). 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.Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo. In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1 h-1), and good oral bioavailability (F: 59%). |
| Animal model | Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models |
| Formulation & Dosage | Dssolved in 10% N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water; ≤3 mg/kg/h; i.v. injection |
| References | J Med Chem. 2007 Nov 1;50(22):5339-56; J Thromb Haemost. 2008 May;6(5):820-9; J Thromb Thrombolysis. 2010 Jan;29(1):70-80. |
