Edoxaban tosylate Monohydrate

製品コードS7280 バッチS728001

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 DMSO 100 mg/mL (135.45 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Edoxaban (DU-176b) は、Kiが0.561 nMで、トロンビンおよびFIXaに対して10,000倍以上の選択性を持つ選択的第Xa因子阻害剤であり、経口投与可能な抗凝固薬でもあります。
in vitro In human plasma, Edoxaban doubles prothrombin time and activates partial thromboplastin time at 0.256 and 0.508 μM, respectively.
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.

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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18624979/

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：

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
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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