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Edoxaban tosylate monohydrate(DU-176b)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Edoxaban tosylate monohydrate(DU-176b)图片
CAS NO:1229194-11-9
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)738.27
FormulaC24H30ClN7O4S.C7H8O3S.H2O
CAS No.1229194-11-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (135.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES CodeO=C(NC1=NC=C(Cl)C=C1)C(N[C@@H]2[C@H](NC(C(S3)=NC4=C3CN(C)CC4)=O)C[C@@H](C(N(C)C)=O)CC2)=O.CC5=CC=C(S(=O)(O)=O)C=C5.[H]O[H]
SynonymsDU176b; DU 176b; Edoxaban; DU-176; DU 176; DU-176b; DU176; Edoxaban tosylate monohydrate, trade name Lixiana.
实验参考方法
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.


Cell Assay: Edoxaban tosylate monohydrate (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 VivoOral 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 modelVenous stasis thrombosis model in rats and rabbits
Formulation & DosageDissolved 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.