受注:045-509-1970 |
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Synonyms | DU-176b | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H30ClN7O4S.C7H8O3S.H2O |
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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 | |||
* <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. |
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. |
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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] |
キナーゼアッセイ | Anti-FXa activity of Edoxaban | |
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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. |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。