Caspofungin Acetate Biological Activity
Rondedzera | Caspofungin Acetate is an antifungal drug inogona kusaita-makwikwi inhibisa kuumbwa kwe1,3-β-d glucan synthase. |
Relatedmapoka | nzira yechiratidzo >> Anti-infective >> Fungus Tsvagiridzo nzvimbo >> Infect |
In vivoresearch | Mbeva dzakaiswa jekiseni ne caspofungin dzakanga dzisina kuchinja kukuru mu ERG waveform yavo pa vitreous concentration ye 0.41 kusvika 4.1 μM, uye retina yavo yakanga isina kuonekwa kuchinja kwe morphological kana kurasikirwa kwesero.Paine vitreous concentration ye41 μM, caspofungin yakaderedza amplitude yemafungu, b wave uye scotopic threshold response yeERG, uye yakakonzerawo kuderera kwenhamba yemasero mu ganglion cell layer [1].Carprofungin (8 mg/kg) kana amphotericin B 1 mg/kg, intraperitoneal jekiseni kamwe chete pazuva 30 h pashure utachiona kwemazuva 7 akatevedzana, maererano motokari kudzora kurapwa, 100% kurarama pazuva 28, zvichiita kuti masikati 100% kufa mwero 11. , mushure mechirwere chetachiona.Kuenzaniswa nekurapa kwekutonga kwemotokari pazuva re5, caspofungin yakaderedza kudzoreredzwa kweCandida inogoneka muitsvo uye uropi matishu apo mutoro wekudzora wakasvika pakakwirira.Mice inobatwa ne caspofungin pachiyero che 2 mg / kg kana yakakwirira yakanga yakaderera zvakanyanya kurongeka kwehuropi pazuva 5 pane mbeva dzakabatwa ne amphotericin B. Amphotericin B uye caspofungin kurapwa kwakaderedza renal fungal mutoro ne 1.7 log CFU / g uye 2.46 kusvika 3.64 log CFU /g, zvichiteerana [2]. |
Mhukaexperiment | Antifungal therapy yakatangwa maawa makumi matatu mushure mechirwere chetachiona uye yakapiwa ne intraperitoneal (ip) jekiseni kamwe pazuva kwemazuva manomwe.Mice dzakabatwa ne1, 2, 4, kana 8 mg / kg / zuva caspofungin, 1 mg / kg / zuva amphotericin B kana kutonga kwemotokari (mvura yakasvibiswa yakasvibiswa).Kubudirira kwemuenzaniso kwakaongororwa nenzira nhatu: nekucherechedza mararamiro ehupenyu hwemhuka dze10 muboka rega rega rekurapa, nekutarisa Candida mutoro muitsvo uye uropi hweboka rechipiri remhuka dzakarapwa, uye nekuongorora histologically itsvo.Uye uropi.Boka rechitatu remhuka dzinorapwa.Mbeva dzakasimbiswa neCO 2 inhalation uye dzakagadzirwa pamaawa makumi matatu (motokari-yakagadziriswa kutonga chete) uye pazuva 5 (maawa makumi maviri nemana mushure me 4th dose), 8 (maawa 24 mushure mekupedzisira dose), uye 14, 21 maawa Uye histological. tissue sampling.(Chete caspofungin kurapwa), uye 28 mushure mekurwisa. |
References | [1].Mojumder DK, et al.Kuongorora retinal toxicity ye intravitreal caspofungin muziso rembeva.Invest Ophthalmol Vis Sci.2010 Nov;51(11):5796-803. [2].Flattery, Amy M. et al.Kubudirira kwe caspofungin mune yechidiki mbeva modhi yepakati tsinga system candidiasis.Antimicrobial Agents uye Chemotherapy (2011), 55 (7), 3491-3497. |
Kemikari uye zvemuviri zvimiro zve caspofungin acetate
Boiling point | 1408.1ºC pa760 mmHg |
Molecular formula | C56H96N10O19 |
Molecular uremu | 1093.31000 |
Hunhu chaihwo | 1092.64000 |
PSA | 412.03000 |
LogP | 0.06150 |
Chitarisiko hunhu | kuchena kune beige |
Mhepo pressure | 0mmHg pa25°C |
Kuchengetedza mamiriro | 20°C |
Kunyungudika kwemvura | H2O: soluble15mg/mL (yakajeka mhinduro) |
Caspofungin Acetate Tsika
Customs code | 2933990099 |
Chinese Overview | 2933990099. Mimwe mishonga yeheterocyclic ine chete nitrogen heteroatoms.Kukosha-yakawedzerwa mutero wemutero: 17.0%.Mutero wekudzoserwa kwemutero: 13.0%.Regulatory mamiriro: Hapana.Inonyanya kufarirwa nyika mutero: 6.5%.General tariff: 20.0% |
Declaration elements | Zita rechigadzirwa, ingredient yemukati, shandisa, hexamethylene chloride, ndapota ratidza chitarisiko, 6-caprolactam, ndapota ratidza chitarisiko, kusaina zuva. |
Summary | 2933990090. heterocyclic compounds nenitrogen hetero-atomu(s) chete.VAT:17.0%.Mutero wekudzoserwa kwemutero: 13.0%..MFN mutero: 6.5%.General tariff:20.0% |
Production Process
Caspofungin inoda kugadzirirwa nekuvirisa semi-synthetic tekinoroji.Chigadzirwa chisina kuchena chemhete huru chinoda kuwanikwa kuburikidza nekuvirisa tekinoroji, uyezve chigadzirwa chepakati chinowanikwa kuburikidza nekuparadzaniswa uye kucheneswa, uyezve chigadzirwa chepakati chinoshandiswa sechinhu chekutanga kupedzisa kupindirana kwecheni padivi uchishandisa tekinoroji yekugadzira kuti uwane pakupedzisira. the target Element.Nekuti iyo "yakaviriswa semi-synthetic" zvigadzirwa zvinoda kuenda kuburikidza neakawanda tekinoroji zvinongedzo senge kuvirisa, kupatsanura uye kucheneswa, synthesis, nezvimwe, iyo tekinoroji nzira uye dhizaini paramende yakaoma kwazvo muChemicalbook.Pamusoro pezvo, izvo zvinodikanwa zvekunyoreswa kwekaspofungin, yakaviriswa semi-synthetic chigadzirwa, zvakare yakakwira zvakanyanya.Mapepa ekunyorera anofanirwa kutanga kubva painovirisa sosi, kwete kungodzidza zvakarongeka kurima kwemhando, tekinoroji yekuvirisa, uye tekinoroji yekuchenesa, asi zvakare kuongorora maitiro ekubatanidza.Nzira, mamiriro, uye kutonga kwetsvina mukuita, nekuti chigadzirwa chekupedzisira hachina kusimba, chero kusangwarira kunodzima zvese zvakamboedza, uye kuoma kwehunyanzvi uye mutengo haukoshi.
Izvo chaizvo nekuda kwezvipingamupinyi zvehunyanzvi uye nzvimbo yakanaka yemakwikwi iyo Hengrui Caspofungin yakachengetedza nzvimbo yakanaka yemutengo mushure mekunyorwa kwayo.
Kudzivirirwa patent kwakapera muna 2014
Kutengeswa kweiyo terminal caspofungin jekiseni munzvimbo dzeruzhinji dzekurapa muChina (chikamu: zviuru gumi yuan)
Kusvika pari zvino, mishonga yemageneric chete yeHengrui Pharmaceuticals, Chia Tai Tianqing, Borui Pharmaceuticals, uye Haisco ndiyo yakatenderwa kunyorwa.Huadong Medicine?
Kambani yekutanga yekutsvagisa yecaspofungin acetate ndeyeMerck, uye manyorerwo emakambani matanhatu ari kuongororwa uye kubvumidzwa, anoti Qilu Pharmaceutical, Nanjing Yinxing Pharmaceutical, Sihuan Pharmaceutical, Osaikang Pharmaceutical, Sino-US Huadong Pharmaceutical, uye Tian Weipharmaceutical Bio.
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...
R&D Chikwata
Jindun Medical ine boka revashandi veR&D nyanzvi, uye inoshandisa nyanzvi zhinji dzemumba nedzekunze dzekugadzira zvinodhaka kutungamira R&D, zvichiita kuti kubatanidza kwedu kuve kwakanyatso uye kushanda zvakanaka.
Isu takabatsira akati wandei epamusoro makambani emishonga emishonga, akadaiHansoh, Hengrui uye HEC Pharm.Pano ticharatidza chikamu chavo.
Customization Case One:
Cas Nha.: 110351-94-5
Customization Nyaya Yechipiri:
Cas Nha.: 144848-24-8
Customization Nyaya Yetatu:
Cas Nha.: 200636-54-0
1.Gadzirisa New Intermediates kana maAPI.Zvakangofanana nepamusoro pekugovanisa kesi, vatengi vane zvinodikanwa kune chaiwo maIntermediates kana APIs, uye havagone kuwana zvigadzirwa zvinodikanwa mumusika, saka isu tinogona kubatsira kuGadzirisa.
2.Process Optimization for Old Products.Chikwata chedu chichabatsira Kukwirisa nekuvandudza kugadzirwa kwakadai nzira yemaitiro yasakara, mutengo wekugadzira wakakwira, uye kushanda kwacho kwakadzikira.Tinogona kupa zvizere zvinyorwa zvekufambisa tekinoroji uye kuvandudzwa kwemaitiro, kubatsira mutengi kuti awedzere kugadzirwa.
Kubva pazvinangwa zvezvinodhaka kusvika kuINDs, JIN DUN Medical inokupa iweimwe-stop personalized R&D mhinduro.
JIN DUN Medical inoomerera pakugadzira timu ine zviroto, kugadzira zvigadzirwa zvine chiremera, zvine hungwaru, zvine hungwaru, uye kuenda zvese kunze kuti uve shamwari yakavimbika uye shamwari yevatengi!