货号:A587736 同义名: 依杜沙班 / DU-176;Savaysa
Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | Factor Xa ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Rivaroxaban |
++
Factor Xa, IC50: 0.7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Apixaban |
++++
Factor Xa (rabbit), Ki: 0.17 nM Factor Xa (human), Ki: 0.08 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Edoxaban tosylate monohydrate |
+++
Factor Xa, Ki: 0.561 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Factor Xa (FXa) is a coagulation factor thrombokinase responsible for the generation of thrombin. Edoxaban is a direct, selective FXa inhibitor with a Ki 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. |
作用机制 | Edoxaban inhibits free FXa by directly binding to FXa without the need of antithrombin, thereby preventing the conversion of prothrombin to thrombin. |
Dose | Rat: 0.3 mg/kg - 3 mg/kg[3] (p.o.) | ||||||||||||||||||||||
Administration | p.o. | ||||||||||||||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00986154 | Venous Thromboembolism ... 展开 >> Deep Vein Thrombosis (DVT) Pulmonary Embolism (PE) Thromboembolism Venous Thrombosis 收起 << | Phase 3 | Completed | - | - |
NCT02219984 | - | Active, not recruiting | July 2019 | Italy ... 展开 >> S. Orsola-Malpighi University hospital Bologna, BO, Italy, 40138 收起 << | |
NCT02611635 | - | Completed | - | Sweden ... 展开 >> Multiple Locations, Sweden 收起 << | |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.82mL 0.36mL 0.18mL |
9.12mL 1.82mL 0.91mL |
18.25mL 3.65mL 1.82mL |
CAS号 | 480449-70-5 |
分子式 | C24H30ClN7O4S |
分子量 | 548.058 |
别名 | 依杜沙班 ;DU-176;Savaysa;DU-176b |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 9 mg/mL(16.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |