|N1-(5-氯吡啶-2-基)-N2-((1S,2R,4S)-4-(二甲基甲酰胺基)-2-(5-甲基-4,5,6,7-四氢噻唑并[5,4-c]吡啶-2-甲酰胺基)环己基)草酰胺4-甲基苯磺酸盐一水合物|CsnPharm

CAS No.: 1229194-11-9

依多沙班对甲苯磺酸盐一水合物 Catalog No. CSN15688

Synonyms: DU-176b monohydrate;DU-176;DU-176b

Edoxaban tosylate 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 drug.

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实验方案

技术信息

生物活性

描述Factor Xa (FXa) is a coagulation factor thrombokinase responsible for the generation of thrombin. Edoxaban Tosylate Monohydrate is the tosylate monohydrate form of Edoxaban. Edoxaban is a direct, selective FXa inhibitor with a K_i value of 0.561nM. In uman plasma samples, the minimum concentrations of edoxaban needed to significantly prolong prothrombin time (PT) and activated partial thromboplastin time were 55 and 50ng/mL, respectively. Plasma edoxaban at the concentration of 5.5 – 1640 ng/ml inhibited the generation of thrombin in a dose-dependent manner. Edoxaban above 10 ng/ml significantly extended the initiation phase of thrombin generation. In human platelet-poor plasma, the peak IC50 value, mRate IC50 value, and endogenous thrombin potential (ETP) IC50 value measured in thrombin generation assay were 0.145, 0.047, and 1.39 µM, respectively. The doses of edoxaban required to reach 50% of inhibition of CT2 lag time and ttPeak were 0.188 and 0.139 µM, respectively. In human platelet-rich plasma, the peak IC50, mRate IC50, and ETP IC50 values were 0.305, 0.230, and 0.636 µM, respectively. In apolipoprotein E (ApoE)-deficient mice, the treatment with 15 mg/kg edoxaban one hour before vascular injury almost completely prevented thrombus formation, and significantly decreased the time to occlusion and the patency rate. The following chronic oral administration of 10 mg/kg edoxaban by gavage b.i.d for six weeks significantly suppressed neointimal hyperplasia.

动物研究

剂量

Rat: 0.1 mg/kg - 2.5 mg/kg^[2] (p.o.); 3 mg/kg - 30 mg/kg^[2] (p.o.) Rabbit: 0.3 mg/kg - 3 mg/kg^[2] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Rats^[3]
Dose	3 mg/kg
Administration	p.o.
T_1/2	3.2 ± 0.4 h (1-12h or 2-12h) 11 ± 6 h (12-24h or 12-48h)
T_max	0.67 ± 0.29 h
C_max	417.2 ± 72.4 ng eq./ml
AUC_0→∞	1.76 ± 0.20 μg eq.·h/ml

参考文献

[1] Mendell J, Noveck RJ, Shi M. Pharmacokinetics of the direct factor Xa inhibitor edoxaban and digoxin administered alone and in combination. J Cardiovasc Pharmacol. 2012 Oct;60(4):335-41.
[2] Furugohri T, Isobe K, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.
[3] DU-176b

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.3545 mL
- 6.7725 mL
- 13.5451 mL
- 5 mM
- 0.2709 mL
- 1.3545 mL
- 2.7090 mL
- 10 mM
- 0.1355 mL
- 0.6773 mL
- 1.3545 mL

技术信息

CAS号

1229194-11-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H40ClN7O8S2

运输

蓝冰

分子量

738.27

别名

DU-176b monohydrate;DU-176;DU-176b;Edoxaban;trade name Lixiana;Savaysa

溶解度

DMSO	98.0 mg/mL (132.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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依多沙班对甲苯磺酸盐一水合物 Catalog No. CSN15688

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