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Fondaparinux sodium

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Chemical Structure| 114870-03-0 同义名 : 磺达肝素(癸)钠 ;Fondaparin sodium;SR-90107A;Fondaparinux (sodium salt);Natural heparin pentasaccharide Sodium;Org 31540
CAS号 : 114870-03-0
货号 : A168977
分子式 : C31H43N3Na10O49S8
纯度 : 98%+
分子量 : 1728.082
MDL号 : MFCD06794972
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 120 mg/mL(69.44 mM),配合低频超声助溶

动物实验配方:
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.
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 <<
实验方案
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

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.