Fondaparinux Biological Activity
Faamatala | Fondaparinux sodium o se mea e faʻalagolago i le antithrombin-faʻalagolago Xa inhibitor. |
Fa'atatauVaega | ala faailo >> Metabolic enzymes/proteases >> Factor Xa Su'esu'ega vaega >> Fa'ama'i fatu |
Sini | Fa'ailoga Xa[1] |
In vitrosu'esu'ega | Fondaparinux sodium o le anticoagulant fou muamua lea e filifilia fa'atatau Xa.Mo Fondaparinux, o le IC50 tau (anti-Xa IU / ml) o monocytes faʻagaoioia (ac-M) o le 0.59 ± 0.05, ma le monocyte-derived particles (MMP) o le 0.17 ± 0.03 [2]. |
I vivosu'esu'ega | Fondaparinux sodium o loʻo i ai se faʻasologa faʻasolosolo, faʻalagolago i fualaʻau pharmacokinetic profile, lea e maua ai se tali sili ona vaʻaia.Fondaparinux sodium o loʻo i ai le 100% bioavailability, e vave ona amata gaioiga, e iai le afa-ola o le 14 i le 16 itula, ma e mafai ona faʻaauau pea ona tetee atu i le thrombosis i totonu ole 24 itula.O le vailaʻau e le aʻafia ai le taimi o le prothrombin poʻo le faʻagaoioia o le taimi o le thromboplastin, e le afaina ai foi le gaioiga poʻo le faʻapipiʻiina o platelet [1]. |
Fa'asinomaga | [1].Bauer KA.ma isi.Fondaparinux sodium: o se inhibitor filifilia o le mea Xa.Am J Health Syst Pharm.2001 Nov 1;58 Suppl 2:S14-7.[2].Ben-Hadj-Khalifa S, et al.Aafiaga faʻalavelave faʻafefete eseʻese o le fondaparinux, enoxaparin ma le heparin e leʻi vaʻaia i faʻataʻitaʻiga sela o le gaosiga o le thrombin.Toto Coagul Fibrinolysis.2011 Iul;22(5):369-73. |
Kemisi ma mea fa'aletino ole Fondaparinux
fua mole | C31H53N3Na10O49S8 |
mamafa mole | 1738.16 |
PSA | 900.82000 |
Fondaparinux o se ituaiga fou o vailaʻau antithrombotic lea ua faʻamaonia e le FDA ina ua maeʻa le heparin ma le maualalo o le molecular weight heparin mo togafitiga ma le puipuia o le tele o arteriovenous thrombosis.
Fa'ailoga: Fondaparinux o lo'o fa'aaogaina mo tagata mama'i o lo'o faia se taotoga tele o vae pito i lalo, e pei o le gau o le suilapalapa, taotoga tele o tulivae po'o le sui o le suilapalapa, e puipuia ai le thromboembolism venous.E faʻaaogaina mo le togafitia o tagata mamaʻi e maua i le angina le mautonu poʻo le faʻaleagaina o le myocardial e le o se ST-segment o loʻo faia faʻanatinati (<120 minute) togafitiga faʻalavelave (PCI) e aunoa ma se faʻamatalaga.E faʻaaogaina mo togafitiga o tagata mamaʻi e maua i le ST-segment elevation myocardial infarction o loʻo faʻaaogaina le thrombolysis poʻo le taimi muamua e le maua ai isi ituaiga o togafitiga toe faʻafoʻi.
1)O le faʻaauau pea o le faʻalauiloaina o maketi a Glaxo o le a tuʻuina ai i le tulaga autu o vailaʻau i le auala faʻafomaʻi a le Matagaluega o le Soifua Maloloina, le toe fuataʻiina o tau o le National Development and Reform Commission, ma le inisiua faafomaʻi a le Matagaluega o Inisiua a Tagata.
A、E le'i ulufale le oloa ile inisiua fa'afoma'i a le atunu'u.I le 2010, o le fetuunaiga o inisiua faafomai faatoa ulufale atu i le inisiua faafomai i le lotoifale o 16 itumalo.O faʻatauga o loʻo i ai i le tulaga muamua ma o le a faasolosolo malie ona suia le maketi o le heparin maualalo-mole-mamafa;itumalo inisiua faafomai: Shaanxi, Shanxi, Inner Mongolia, Liaoning, Tibet, Yunnan, Guangdong , Guangxi, Hainan, Jiangsu, Gansu, Fujian, Jiangxi, Henan, Hubei, Beijing.
B、O faʻailoga o loʻo faʻateleina pea.GSK i le taimi nei e 3 faʻailoga i le falemaʻi.Mo se faʻataʻitaʻiga, o faʻailoga mo stent e faʻamaonia faapitoa.E le maua isi heparins.Ole fa'aogaina ole fa'aoga ole stent e fa'atupula'ia ile 30% i tausaga ta'itasi.Faatasi ai ma le faʻatagaina o faʻailoga fou, o le a faʻateleina le faʻatau.I le talitonuga, o faʻamaʻi uma e togafitia e oloa faʻasologa o le heparin e mafai ona togafitia e lenei oloa.
C, tau lelei, o le tau maualalo o lenei oloa i le maketi a Amerika e 132 US tala taʻitasi, i Saina o le 168 yuan, o le tau i totonu o le atunuu o le a le pa'ū.Afai e te auina atu i fafo, o le maketi faava o malo e lautele avanoa;
2) O le tulaga faʻapitoa e maualuga, o mea mataʻutia o loʻo faʻapipiʻiina i 75 laasaga, ma ua maeʻa le pateni mo le 5 tausaga (tusia i le 2014).E leʻi faʻatagaina e isi tagata gaosi oloa.O le tu'ufa'atasiga e matua faigata lava.O le a le faia i lalo ifo o le 10 tausaga.O le taamilosaga e umi, faigata, ma tupe teu.maualuga.E toalaiti tagata tauva i totonu o le atunuu, ma o tagata tauva mai fafo e maualuga le tau o meafaitino.O la matou sini o le faʻaauau pea ona faʻaitiitia tau o mea mataʻutia ma sui Glaxo i le gaosiga o mea mata.
Hengrui Pharmaceuticals Fondaparinux na faʻamaonia e avea ma faʻataʻitaʻiga muamua i Saina 2018.
Guangdong Runxing Biotechnology Co., Ltd. o loʻo i ai se galuega faʻaletausaga o le 210 kilokalama o le fondaparinux sodium advanced intermediate N3, lea o le a faila i le 2018.
Fondaparinux na muamua fausia e MYLAN IRELAND.I le taimi nei, Hengrui Pharmaceuticals, Borui Pharmaceuticals, Haisco.
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FA'ATAITAI O GALUEGA
●Mata'u maualuga Catalytic Hydrogenation .High Pressure Hydrogenolysis Reaction .Cryogenic Reaction (<-78%C)
●Aromatic Heterocyclic Synthesis
●Toe Fa'atonuga
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Gignard Reaction
Meafaigaluega
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Fa'asinomaga Tulaga Muamua:
Kase Numera: 110351-94-5
Tulaga Fa'apitoa Lua:
Cas Nu.: 144848-24-8
Tulaga Fa'apitoa Tolu:
Cas Nu.: 200636-54-0
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