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首页 / 抑制剂/激动剂 / 代谢酶 / Factor Xa / Edoxaban/依度沙班

Edoxaban/依度沙班 {[allProObj[0].p_purity_real_show]}

货号：A587736 同义名： 依杜沙班 / DU-176; Savaysa

Edoxaban是一种口服活性因子 Xa 抑制剂，对人游离 FXa 的 Ki 值为 0.561 nM。它被用于预防和治疗静脉血栓栓塞性疾病，并在临床试验中显示了其优越的抗凝血性能。

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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+
Edoxaban/依度沙班 化学结构 CAS号：480449-70-5
Edoxaban/依度沙班 化学结构
CAS号：480449-70-5
Edoxaban/依度沙班 3D分子结构
CAS号：480449-70-5
Edoxaban/依度沙班 化学结构 CAS号：480449-70-5
Edoxaban/依度沙班 3D分子结构 CAS号：480449-70-5
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Edoxaban/依度沙班 纯度/质量文件 产品仅供科研

货号：A587736 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Factor Xa ↓ 其他靶点 纯度
Rivaroxaban ++

Factor Xa, IC50: 0.7 nM

 		98%
Apixaban ++++

Factor Xa (rabbit), Ki: 0.17 nM

Factor Xa (human), Ki: 0.08 nM

 		98%
Edoxaban tosylate monohydrate +++

Factor Xa, Ki: 0.561 nM

 		98+%
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。

Edoxaban/依度沙班 生物活性

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.

Edoxaban/依度沙班 细胞实验

Cell Line
Concentration Treated Time Description References
Human Umbilical Vein Endothelial Cells (HUVECs) 1 nM-1 μM Edoxaban alone promoted cell viability and growth. In FXa-treated ECs, edoxaban showed anti-inflammatory properties by blocking PBMC and platelet adhesion to HUVECs, while effectively reversing the transmigration of PBMCs through HUVECs monolayers caused by FXa. Edoxaban also protected the endothelium by attenuating FXa-induced migration in a wound healing assay and by partially neutralizing the anti-angiogenic effects of FXa. Front Pharmacol. 2023 Sep 29;14:1244098.

Edoxaban/依度沙班 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Male C57Bl/6N mice Transient middle cerebral artery occlusion model Oral gavage 3.3 mg/kg body weight Three administrations (72, 48, and 24 hours before tMCAO) To assess the protective mechanism of edoxaban in a model of ischemia/reperfusion injury, results showed that edoxaban significantly reduced infarct volumes, improved neurological outcome, and attenuated brain tissue inflammation. Int J Mol Sci. 2021 Sep 13;22(18):9893
C57B/6J mice Atrial fibrillation model Oral 0.03 mg/d Once daily for 14 days Evaluate the effect of edoxaban on atrial fibrillation and coagulation Front Pharmacol. 2022 Jun 3;13:904317

Edoxaban/依度沙班 动物研究

Dose Rat: 0.3 mg/kg - 3 mg/kg[3] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[4]
Dose 1 mg/kg
Administration p.o. or i.v.
AUC0→24h 212 ± 87 ng·h/ml (p.o.)
545 ± 21 ng·h/ml (i.v.)
AUC0-inf 301 ng·h/ml (p.o.)
539 ± 29 ng·h/ml (i.v.)
T1/2 4.85 ± 2.88 h (p.o.)
1.32 ± 0.69 h (i.v.)
Tmax 0.500 ± 0.000 h (p.o.)
AUClast 184 ± 94 ng·h/ml (p.o.)
516 ± 29 ng·h/ml (i.v.)
CL 1.86 ± 0.10 L/h/kg (i.v.)
Cmax 72.7 ± 35.7 ng/ml (p.o.)
Vss 2.14 ± 0.36 L/kg (i.v.)

Edoxaban/依度沙班 临床研究

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 <<

Edoxaban/依度沙班 参考文献

[1]Goette A, Merino JL, et al. Edoxaban versus enoxaparin-warfarin in patients undergoing cardioversion of atrial fibrillation (ENSURE-AF): a randomised, open-label, phase 3b trial. Lancet. 2016 Oct 22;388(10055):1995-2003.

[2]Bounameaux H, Camm AJ. Edoxaban: an update on the new oral direct factor Xa inhibitor. Drugs. 2014 Jul;74(11):1209-31.

[3]Morishima Y, Honda Y, et al. Prevention of Stent Thrombosis in Rats by a Direct Oral Factor Xa Inhibitor Edoxaban. Pharmacology. 2019;103(1-2):17-22.

[4]DU-176

Edoxaban/依度沙班 实验方案

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

Edoxaban/依度沙班 技术信息

CAS号480449-70-5
分子式C24H30ClN7O4S
分子量 548.06
SMILES Code CN1CCC2=C(SC(C(N[C@@H]3C[C@@H](C(N(C)C)=O)CC[C@@H]3NC(C(NC4=NC=C(Cl)C=C4)=O)=O)=O)=N2)C1
MDL No. MFCD13195544
别名 依杜沙班 ;DU-176; Savaysa; DU-176b
运输蓝冰
InChI Key HGVDHZBSSITLCT-JLJPHGGASA-N
Pubchem ID 10280735
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Edoxaban | 480449-70-5 | DU-176 | DU176 | DU 176 | FXa Inhibitor | Metabolic Enzyme/Protease | Factor Xa | Thrombin | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Edoxaban/依度沙班 纯度/质量文件 | Edoxaban/依度沙班 亚型比较 | Edoxaban/依度沙班 生物活性 | Edoxaban/依度沙班 动物研究 | Edoxaban/依度沙班 临床数据 | Edoxaban/依度沙班 参考文献 | Edoxaban/依度沙班 实验方案 | Edoxaban/依度沙班 技术信息

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