I-Fondaparinux Biological Activity
Chaza | I-Fondaparinux sodium iyi-antithrombin-dependent factor Xa inhibitor. |
OkuhlobeneIzigaba | indlela yesignali >> Ama-enzyme/amaphrotheni e-metabolic >> Izindawo zokucwaninga nge-Factor Xa >> Izifo zenhliziyo |
Ithagethi | I-Factor Xa[1] |
In vitroizifundo | I-Fondaparinux sodium iyi-anticoagulant yokuqala entsha eqondisa ngokukhetha i-factor Xa.Ku-Fondaparinux, inani le-IC50 (anti-Xa IU/ml) lama-monocyte acushiwe (ac-M) lingu-0.59±0.05, kanye nezinhlayiya ezitholakala ku-monocyte (MMP) ngu-0.17±0.03 [2]. |
Nge-vivoucwaningo | I-Fondaparinux sodium inephrofayili ye-pharmacokinetic eqondile, encike kumthamo, enikeza impendulo ebikezelwe kakhulu.I-Fondaparinux sodium ine-bioavailability engu-100%, iqala ngokushesha ukusebenza, inesigamu sempilo yamahora angu-14 kuya kwangu-16, futhi ingaqhubeka nokumelana ne-thrombosis phakathi namahora angu-24.Umuthi asithinti isikhathi se-prothrombin noma isikhathi esicushiwe se-thromboplastin, futhi asithinti ukusebenza kweplatelet noma ukuhlanganisa [1]. |
Izithenjwa | [1].Bauer KA.et al.I-Fondaparinux sodium: inhibitor ekhethiwe ye-factor Xa.Am J Health Syst Pharm.2001 Nov 1;58 Isengezo 2:S14-7.[2].Ben-Hadj-Khalifa S, et al.Umphumela ohlukile we-coagulation inhibitory we-fondaparinux, i-enoxaparin ne-heparin engahlukanisiwe kumamodeli wamaseli esizukulwane se-thrombin.Igazi Coagul Fibrinolysis.2011 Jul;22(5):369-73. |
Izakhiwo zamakhemikhali nezomzimba ze-Fondaparinux
Ifomula yamangqamuzana | I-C31H53N3Na10O49S8 |
Isisindo samangqamuzana | 1738.16 |
I-PSA | 900.82000 |
I-Fondaparinux iwuhlobo olusha lomuthi we-antithrombotic ogunyazwe yi-FDA ngemuva kwe-heparin kanye ne-heparin yesisindo esiphansi samangqamuzana okwelapha nokuvimbela izinhlobonhlobo ze-arteriovenous thrombosis.
Izinkomba: I-Fondaparinux isetshenziselwa iziguli ezihlinzwa kakhulu ngamathambo ezitho ezingezansi, njengokuphuka kwe-hip, ukuhlinzwa okukhulu kwamadolo noma ukushintshwa kwe-hip, ukuvimbela i-venous thromboembolism.Isetshenziselwa ukwelapha iziguli ezine-angina engazinzile noma i-non-segment elevation myocardial infarction ezithola ukwelashwa okuphuthumayo (ngaphansi kwemizuzu engu-120) (PCI) ngaphandle kwenkomba.Isetshenziselwa ukwelapha iziguli ezine-ST-segment elevation myocardial infarction ezisebenzisa i-thrombolysis noma ekuqaleni ezingatholi ezinye izinhlobo zokwelapha kabusha.
1)Ukuphromotha kwemakethe okuqhubekayo kuka-Glaxo kuzoyibeka endaweni eyinhloko yezidakamizwa endleleni elandelayo yomtholampilo yoMnyango Wezempilo, ukuguqulwa kwamanani entengo yeKhomishini Kazwelonke Yokuthuthukiswa Nezinguquko, kanye nomshwalense wezokwelapha woMnyango Wezomshuwalense Wabantu.
A, Umkhiqizo awukakangeni kumshwalense wezempilo kazwelonke.Ngo-2010, ukulungiswa komshwalense wezokwelapha kusanda kungena kumshwalense wendawo wezokwelapha wezifundazwe eziyi-16.Ukuthengisa kusesigabeni sokuqala futhi kancane kancane kuzongena esikhundleni semakethe ye-heparin enesisindo esiphansi;izifundazwe zomshuwalense wezokwelapha: Shaanxi, Shanxi, Inner Mongolia, Liaoning, Tibet, Yunnan, Guangdong , Guangxi, Hainan, Jiangsu, Gansu, Fujian, Jiangxi, Henan, Hubei, Beijing.
B, Izinkomba zisakhula.I-GSK njengamanje inezinkomba ezi-3 emtholampilo.Isibonelo, izinkomba zama-stents zigunyazwe kuphela.Amanye ama-heparin awatholakali.Ukusetshenziswa komtholampilo kwama-stents kukhuphuka ngo-30% njalo ngonyaka.Ngokugunyazwa kwezinkomba ezintsha, ukuthengisa kuzokhula.Ngokombono, zonke izifo eziphathwa ngemikhiqizo yochungechunge lwe-heparin zingelashwa yilo mkhiqizo.
C、Inzuzo yentengo, inani elincane lentengo yalo mkhiqizo emakethe yase-US ingamadola ayi-132 lilinye, eChina lingu-168 yuan, intengo yasekhaya ngeke yehle.Uma uthumela ngaphandle, imakethe yamazwe ngamazwe inendawo ebanzi;
2) Umkhawulo wezobuchwepheshe uphakeme, impahla eluhlaza ihlanganiswa ngezinyathelo ezingu-75, futhi ilungelo lobunikazi liphelelwe yisikhathi iminyaka engu-5 (i-athikili ngo-2014).Ayigunyazwanga abanye abakhiqizi.I-synthesis inzima kakhulu.Ngeke kwenziwe ngaphansi kweminyaka eyi-10.Umjikelezo mude, unzima, futhi utshale imali.phezulu.Bambalwa abancintisana nabo basekhaya, futhi izimbangi zakwamanye amazwe zinezindleko eziphezulu zempahla eluhlaza.Umgomo wethu uwukunciphisa ngokuqhubekayo izindleko zempahla eluhlaza futhi esikhundleni se-Glaxo ekukhiqizeni impahla eluhlaza.
I-Hengrui Pharmaceuticals Fondaparinux yavunywa njengokulingisa kokuqala e-China 2018.
I-Guangdong Runxing Biotechnology Co., Ltd. inomkhiqizo wonyaka wama-210 kg we-fondaparinux sodium advanced intermediate N3, ezofakwa ngo-2018.
I-Fondaparinux ekuqaleni yasungulwa yi-MYLAN IRELAND.Njengamanje, i-Hengrui Pharmaceuticals, i-Borui Pharmaceuticals, i-Haisco.
I-JIN DUN Medical ineIziqu ze-ISO futhi ihlangabezana namazinga okukhiqiza e-GMP, kuqashwe ochwepheshe basekhaya nabangaphandle abanolwazi olunzulu lokuqondisa i-R&D yenkampani.
TECHNOL OGY UBUHLE
●I-High Pressure Catalytic Hydrogenation.I-High Pressure Hydrogenolysis Reaction .Ukusabela kwe-Cryogenic (<-78%C)
● I-Aromatic Heterocyclic Synthesis
●Ukusabela Kabusha
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Ukusabela kukaGiignard
Izisetshenziswa
Ilebhu yethu inezinsiza ezihlukahlukene zokuhlola nokuhlola, njenge: NMR (Bruker 400M), HPLC、chiral-HPLC、LC-MS、LC-MS/MS (API 4000),IR,UV,GC,GC,GC-MS, Chromatography, I-Microwave Synthesizer, i-Parallel Synthesizer, i-Differential Scanning Calorimeter (DSC), i-Electron Microscope...
Ithimba le-R&D
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Sisize izinkampani ezimbalwa eziphezulu zasekhaya ezithaka imithi, njengeI-Hansoh, i-Hengrui ne-HEC Pharm.Lapha sizokhombisa ingxenye yazo.
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Ikesi Lokwenza Ngokwezifiso:
Inombolo yeCas: 144848-24-8
Ikesi Lesithathu Lokwenza Ngokwezifiso:
Inombolo yeCas: 200636-54-0
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