product name Edoxaban
Description: Edoxaban (also known as DU-176b) is a potent, selective, orally bioavailable factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is used as an anticoagulant drug. Edoxaban acts as a direct factor Xa inhibitor. It was developed by Daiichi Sankyo and was approved in July 2011 in Japan for prevention of venous thromboembolisms (VTE) following lower-limb orthopedic surgery. It was also approved by the FDA in January 2015 for the prevention of stroke and non–central-nervous-system systemic embolism.
References: J Thromb Haemost. 2008 Sep;6(9):1542-9.
548.06
Formula
C24H30ClN7O4S
CAS No.
480449-70-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
DU-176b
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19420088
| In Vitro |
In vitro activity: In human plasma, Edoxaban doubles prothrombin time and activates partial thromboplastin time at 0.256 and 0.508 μM, respectively. Kinase Assay: Cell Assay: Edoxaban (DU-176b) inhibited FXa with Ki values of 0.561 nM for free FXa, 2.98 nM for prothrombinase, and exhibited >10 000-fold selectivity for FXa. DU-176b doubled prothrombin time and activated partial thromboplastin time in human plasma. DU-176b did not impair platelet aggregation by ADP, collagen or U46619 . |
|---|---|
| In Vivo | Oral administration of Edoxaban produces potent anti-Xa activity and high drug concentration in plasma in rats and monkeys. In vivo, Edoxaban dose-dependently inhibits thrombus formation in rat and rabbit thrombosis models. |
| Animal model | Venous stasis thrombosis model in rats and rabbits |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose; 0.3–3 mg/kg (Rabbit); 0.5–12.5 mg/kg (Rat); oral gavage |
| References | J Thromb Haemost. 2008 Sep;6(9):1542-9. |
