Fondaparinux Biological Activity
Rondedzera | Fondaparinux sodium inonzi antithrombin-inotsamira chinhu Xa inhibitor. |
RelatedCategories | nzira yechiratidzo >> Metabolic enzymes/proteases >> Factor Xa Research nzvimbo >> Zvirwere zvemoyo |
Target | Factor Xa[1] |
In vitrozvidzidzo | Fondaparinux sodium ndiyo yekutanga anticoagulant itsva inonangana nechinhu Xa.Kune Fondaparinux, iyo IC50 kukosha (anti-Xa IU/ml) ye activated monocytes (ac-M) i 0.59±0.05, uye monocyte-inotorwa particles (MMP) i 0.17±0.03 [2]. |
In vivoresearch | Fondaparinux sodium ine mutsara, dosi-inotsamira pharmacokinetic mbiri, iyo inopa mhinduro inofanotaurwa.Fondaparinux sodium ine 100% bioavailability, ine kukurumidza kutanga kwekuita, ine hafu yehupenyu hwemaawa gumi nemana kusvika ku16, uye inogona kuramba ichidzivisa thrombosis mukati maawa makumi maviri nemana.Mushonga haukanganisi nguva yeprothrombin kana kuti yakagadziriswa chikamu che thromboplastin nguva, uye haina kukanganisa kushanda kweplatelet kana kuunganidza [1]. |
References | [1].Bauer KA.et al.Fondaparinux sodium: a selective inhibitor ye factor Xa.Am J Health Syst Pharm.2001 Nov 1;58 Suppl 2:S14-7.[2].Ben-Hadj-Khalifa S, nevamwe.Differential coagulation inhibitory effect ye fondaparinux, enoxaparin uye unfractionated heparin mumasero emhando ye thrombin generation.Ropa Coagul Fibrinolysis.2011 Jul;22(5):369-73. |
Kemikari uye zvemuviri zvimiro zveFondaparinux
Molecular formula | C31H53N3Na10O49S8 |
Molecular uremu | 1738.16 |
PSA | 900.82000 |
Fondaparinux rudzi rutsva rweantithrombotic drug yakabvumidzwa neFDA mushure meheparin uye yakaderera molecular weight heparin yekurapa nekudzivirira kwakasiyana arteriovenous thrombosis.
Zviratidzo: Fondaparinux inoshandiswa kune varwere vari kuvhiyiwa kukuru kwemapfupa emakumbo ezasi, zvakadai sekuputsika kwehudyu, kuvhiyiwa kukuru kwemabvi kana kuchinjwa kwehudyu, kudzivirira venous thromboembolism.Inoshandiswa pakurapa kwevarwere vane angina isina kugadzikana kana kuti isiri-ST-segment elevation myocardial infarction inopinda nokukurumidza (<120 maminitsi) invasive treatment (PCI) pasina chiratidzo.Inoshandiswa pakurapa varwere vane ST-segment elevation myocardial infarction vanoshandisa thrombolysis kana pakutanga vasingagamuchire mamwe maitiro ekurapazve.
1)Glaxo inoenderera mberi yekusimudzira musika ichaiisa munzvimbo yepakati pezvinodhaka munzira inotevera yekiriniki yeBazi rezvehutano, shanduko yemitengo yeNational Development and Reform Commission, uye inishuwarenzi yekurapa yeBazi rePeople's Inishuwarenzi.
A、Chigadzirwa hachisati chapinda muinishuwarenzi yenyika.Muna 2010, gadziriso yeinishuwarenzi yekurapa ichangopinda muinishuwarenzi yemunharaunda yematunhu gumi nematanhatu.Kutengesa kuri padanho rekutanga uye zvishoma nezvishoma kutsiva yakaderera-molecular-uremu heparin musika;mapurovhinzi einishuwarenzi yezvokurapa: Shaanxi, Shanxi, Inner Mongolia, Liaoning, Tibet, Yunnan, Guangdong , Guangxi, Hainan, Jiangsu, Gansu, Fujian, Jiangxi, Henan, Hubei, Beijing.
B, Zvinoratidza zvichiri kuwedzera.GSK parizvino ine 3 zviratidzo mukiriniki.Semuenzaniso, zviratidzo zve stents zvinotenderwa chete.Mamwe maheparin haawaniki.Kushandiswa kwekiriniki kwema stents kunowedzera ne30% gore negore.Nekubvumirwa kwezviratidzo zvitsva, kutengesa kuchawedzera.Mune dzidziso, zvirwere zvese zvinorapwa neheparin akatevedzana zvigadzirwa zvinogona kurapwa nechigadzirwa ichi.
C、Mutengo wakanakira, mutengo wakaderera wechigadzirwa ichi mumusika weUS madhora zana nemakumi matatu nemaviri emadhora, muChina i168 yuan, mutengo wepamba hauzodonha.Kana iwe uchiita kunze kwenyika, musika wepasi rose une nzvimbo yakafara;
2) Chikumbaridzo chehunyanzvi chakakwira, iyo mbishi inogadzirwa mumatanho makumi manomwe neshanu, uye patent yapera kwemakore mashanu (chinyorwa muna 2014).Izvo hazvina kubvumidzwa nevamwe vanogadzira.Iyo synthesis yakaoma zvakanyanya.Hazvizoitwe mukati memakore asingasviki gumi.Kutenderera kwakareba, kwakaoma, uye kuisa mari.high.Kune vashoma vakwikwidzi vemumba, uye vakwikwidzi vekunze vane mitengo yakakwira yezvigadzirwa.Chinangwa chedu ndechekuramba tichidzikisira mutengo wemidziyo uye kutsiva Glaxo mukugadzirwa kwezvinhu.
Hengrui Pharmaceuticals Fondaparinux yakabvumidzwa seyekutanga kutevedzera muChina 2018.
Guangdong Runxing Biotechnology Co., Ltd. ine gore negore kuburitsa kwe210 kg ye fondaparinux sodium yepamusoro yepakati N3, iyo ichaiswa muna 2018.
Fondaparinux yakatanga kugadzirwa neMYLAN IRELAND.Parizvino, Hengrui Pharmaceuticals, Borui Pharmaceuticals, Haisco.
JIN DUN Medical aneISO qualification uye inosangana neGMP yekugadzira zviyero, vakashandirwa mudzimba nevekunze nyanzvi dzekugadzira zvinodhaka vane ruzivo rwakapfuma kutungamira R&D yekambani.
TECHNOL OGY ADVANTAGES
●High Pressure Catalytic Hydrogenation .High Pressure Hydrogenolysis Reaction .Cryogenic Reaction (<-78%C)
●Aromatic Heterocyclic Synthesis
● Rearrangement Reaction
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Gignard Reaction
Equipments
Yedu Lab ine midziyo yakasiyana-siyana yekuedza uye yekuedza, yakadai se: NMR (Bruker 400M), HPLC, chiral-HPLC, LC-MS, LC-MS/MS (API 4000), IR, UV, GC, GC-MS, Chromatography, Microwave Synthesizer, Parallel Synthesizer, Differential Scanning Calorimeter (DSC), Electron Microscope...
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Isu takabatsira akati wandei epamusoro makambani emishonga emishonga, akadaiHansoh, Hengrui uye HEC Pharm.Pano ticharatidza chikamu chavo.
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