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磺达肝癸钠 /Fondaparinux sodium {[allProObj[0].p_purity_real_show]}

货号:A168977 同义名: 磺达肝素(癸)钠 / Fondaparin sodium;SR-90107A

Fondaparinux sodium is a pentasaccharide inhibitor of antithrombin-dependent factor Xa (IC50 = 40 nM). It can bind to antithrombin III.

Fondaparinux sodium 化学结构 CAS号:114870-03-0
Fondaparinux sodium 化学结构
CAS号:114870-03-0
Fondaparinux sodium 3D分子结构
CAS号:114870-03-0
Fondaparinux sodium 化学结构 CAS号:114870-03-0
Fondaparinux sodium 3D分子结构 CAS号:114870-03-0
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Fondaparinux sodium 纯度/质量文件 产品仅供科研

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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。

Fondaparinux sodium 生物活性

描述 The activated serine protease Factor Xa (FXa), activated by both the intrinsic and the extrinsic pathways, plays a central role in the blood coagulation cascade. FXa catalyzes the conversion of prothrombin tothrombin through the prothrombinase complex[3]. Fondaparinux Sodium is a pentasaccharide inhibitor of antithrombin-dependent factor Xa with IC50 of 40 nM. Subcutaneous doses of 2.5 mg of fondaparinux once daily for at least five days reduced venous thromboembolism risk in patients undergoing surgery for fracture by 56.4 percent[4]. Fondaparinux inhibited endogenous FXa activity in platelet-poor human plasma with IC50 of 11 nM and 19 nM in rat plasma, whereas fondaparinux showed no significant inhibition of platelet-associated thrombin generation at the highest concentration tested (IC50 >300 nM) in rat model of balloon injury[5].
作用机制 Fondaparinux Sodium binds to antithrombin and induces a conformational change in the antithrombin molecule, creating an increased affinity for factor Xa and causing a several thousand-fold increase in the inhibition of factor Xa by antithrombin.

Fondaparinux sodium 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
NCT01178333 - Completed - United States, Iowa ... 展开 >> University of Iowa Iowa City, Iowa, United States, 52242 United States, Louisiana Tulane University New Orleans, Louisiana, United States, 70112 United States, Maryland University of Maryland Greenebaum Cancer Center Baltimore, Maryland, United States, 21201 Johns Hopkins Baltimore, Maryland, United States, 21205 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Children's Hospital, Boston Boston, Massachusetts, United States, 02115 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, New York Cornell University New York, New York, United States, 10065 United States, North Carolina University of North Carolina, Chapel Hill Chapel Hill, North Carolina, United States, 27599 Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Case Western Reserve University School of Medicine Cleveland, Ohio, United States, 44106 Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Washington Fred Hutchinson Cancer Research Center Seattle, Washington, United States, 98104 United States, Wisconsin Gunderson Clinic LaCrosse, Wisconsin, United States, 54601 University of Wisconsin Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 Froedtert Milwaukee, Wisconsin, United States, 53201 St. Luke's Medical Center Milwaukee, Wisconsin, United States, 53215 收起 <<
NCT01178333 - Completed - -
NCT00127855 Haemophilus Influenzae Type b ... 展开 >> Neisseria Meningitidis 收起 << Phase 2 Completed - Australia, South Australia ... 展开 >> GSK Investigational Site North Adelaide, South Australia, Australia, 5006 Australia, Victoria GSK Investigational Site Carlton, Victoria, Australia, 3053 Australia, Western Australia GSK Investigational Site Subiaco, Western Australia, Australia, 6018 收起 <<

Fondaparinux sodium 参考文献

[1]Robinson DM, Wellington K. Fondaparinux sodium: a review of its use in the treatment of acute venous thromboembolism. Am J Cardiovasc Drugs. 2005;5(5):335-46.

[2]Bauer KA. Fondaparinux sodium: a selective inhibitor of factor Xa. Am J Health Syst Pharm. 2001 Nov 1;58 Suppl 2:S14-7.

[3]Roehrig S, Straub A, Pohlmann J, Lampe T, Pernerstorfer J, Schlemmer KH, Reinemer P, Perzborn E. Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. J Med Chem. 2005 Sep 22;48(19):5900-8. doi: 10.1021/jm050101d. PMID: 16161994.

[4]Eriksson BI, Bauer KA, Lassen MR, Turpie AG; Steering Committee of the Pentasaccharide in Hip-Fracture Surgery Study. Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip-fracture surgery. N Engl J Med. 2001 Nov 1;345(18):1298-304. doi: 10.1056/NEJMoa011100. PMID: 11794148.

[5]Gerotziafas GT, Galea V, Mbemba E, Sassi M, Roman MP, Khaterchi A, van Dreden P, Japcowitz M, Lotz JP, Bernaudin JF, Fareed J, Hatmi M, Elalamy I. Effect of low molecular weight heparins and fondaparinux upon thrombin generation triggered by human pancreatic cancer cells BXPC3. Curr Vasc Pharmacol. 2014;12(6):893-902. doi: 10.2174/157016111206141210121441. PMID: 22724467.

Fondaparinux sodium 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.58mL

0.12mL

0.06mL

2.89mL

0.58mL

0.29mL

5.79mL

1.16mL

0.58mL

Fondaparinux sodium 技术信息

CAS号114870-03-0
分子式C31H43N3Na10O49S8
分子量 1728.082
别名 磺达肝素(癸)钠 ;Fondaparin sodium;SR-90107A;Fondaparinux (sodium salt);Natural heparin pentasaccharide Sodium;Org 31540
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

H2O: 120 mg/mL(69.44 mM),配合低频超声助溶

动物实验配方
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