Edoxaban tosylate Monohydrate

製品コードS7280 バッチS728002

印刷

化学情報

Chemical Structure Synonyms DU-176b Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H30ClN7O4S.C7H8O3S.H2O
分子量 738.27 CAS No. 1229194-11-9
Solubility (25°C)* 体外  
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明 Edoxaban (DU-176b) 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.
in vitro In human plasma, Edoxaban doubles prothrombin time and activates partial thromboplastin time at 0.256 and 0.508 μM, respectively. [1]
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. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Anti-FXa activity of Edoxaban
FXa is added to the mixture of Edoxaban or 5% DMSO control and a chromogenic substrate S-2222 (250–1000 μM) in a reaction buffer (20 mm Tris–HCl, pH 7.4, 150 mm NaCl, 0.1% BSA). The final concentrations of FXa are as follows: human FXa (0.005 U/mL, 0.7 nM), rabbit FXa (0.005 U/mL, molarity unavailable), rat FXa (0.025 U/mL, 10 nM) and cynomolgus monkey FXa (0.025 U/mL, 3 nM). To measure amidolysis of S-2222 by FXa, the absorbance at 405 nm is monitored with a microplate spectrophotometer SPECTRAmax 340 at 30 °C for 10 min and the reaction velocity (mO.D./min) is obtained. The inhibition constant (Ki) values of Edoxaban are calculated by the Lineweaver–Burk plots and subsequent secondary plots.
動物実験 動物モデル Venous stasis thrombosis model in rats and rabbits
投薬量 0.3–3 mg/kg (Rabbit); 0.5–12.5 mg/kg (Rat)
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays [ J Thromb Haemost, 2020, 18(8):1866-1873] PubMed: 32294291
The Anticoagulant Nafamostat Potently Inhibits SARS-CoV-2 S Protein-Mediated Fusion in a Cell Fusion Assay System and Viral Infection In Vitro in a Cell-Type-Dependent Manner [ Viruses, 2020, 10;12(6):E629] PubMed: 32532094
Simple LC-MS/MS method using core-shell ODS microparticles for the simultaneous quantitation of edoxaban and its major metabolites in human plasma [ J Chromatogr B Analyt Technol Biomed Life Sci, 2020, 1146:122121] PubMed: 32361632
The anticoagulant nafamostat potently inhibits SARS-CoV-2 infection in vitro: an existing drug with multiple possible therapeutic effects [ bioRxiv, 2020, 10.1101/2020.04.22.054981] PubMed: None
Effects of the oral, direct factor Xa inhibitor edoxaban on routine coagulation assays, lupus anticoagulant and anti-Xa assays [ Scand J Clin Lab Invest, 2018, 78(7-8):575-583] PubMed: 30278787
Edoxaban: Impact on routine and specific coagulation assays. A practical laboratory guide [ Thromb Haemost, 2016, 115(2):368-81] PubMed: 26510969

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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