I-Caspofungin Acetate Biological Activity
Chaza | I-Caspofungin Acetate iyisidakamizwa se-antifungal esingakwazi ukuvimbela ngokungenakuncintisana ukuhlanganiswa kwe-1,3-β-d glucan synthase. |
Okuhlobeneizigaba | indlela yesignali >> Anti-infective >> Isikhunta Izindawo zocwaningo >> Thelela |
Nge-vivoucwaningo | Amagundane ajovwe nge-caspofungin ayengenazo izinguquko eziphawulekayo ku-waveform yawo ye-ERG ekuhlanganiseni kwe-vitreous kuka-0.41 kuya ku-4.1 μM, futhi i-retina yawo yayingenazo izinguquko ezibonakalayo ze-morphological noma ukulahlekelwa kweseli.Ekuhlanganiseni kwe-vitreous kwe-41 μM, i-caspofungin yehlise ukuphakama kwegagasi, i-b wave kanye ne-scotopic threshold response ye-ERG, futhi yabangela ukwehla kwenani lamaseli kungqimba lweseli ye-ganglion [1].I-Carprofungin (8 mg/kg) noma i-amphotericin B 1 mg/kg, umjovo we-intraperitoneal kanye ngosuku emahoreni angama-30 ngemva kokutheleleka izinsuku ezingu-7 zilandelana, uma kuqhathaniswa nokuphathwa kokulawulwa kwemoto, ukusinda okungu-100% ngosuku lwama-28, okuholela ekufeni kwabantu abangu-100% emini kwayi-11. , ngemva kwenselele yokutheleleka.Uma kuqhathaniswa nokwelashwa kokulawula imoto ngosuku lwe-5, i-caspofungin yehlisa ukutholwa kwe-Candida esebenzayo ezinso nasezicubu zobuchopho lapho umthwalo wokulawula ufinyelela inani eliphakeme.Amagundane aphathwe nge-caspofungin ngomthamo we-2 mg/kg noma ngaphezulu abe nomthwalo wobuchopho ophansi kakhulu ngosuku lwe-5 kunamagundane aphathwe i-amphotericin B. I-Amphotericin B kanye nokwelashwa kwe-caspofungin kwehlise umthwalo wesikhunta ezinso ngo-1.7 log CFU/g kanye ne-2.46 kuya ku-3.64 log CFU /g, ngokulandelana [2]. |
Isilwaneukuhlola | Ukwelashwa kwe-antifungal kwaqalwa emahoreni angama-30 ngemuva kwenselele yokutheleleka futhi kwanikezwa ngomjovo we-intraperitoneal (ip) kanye ngosuku izinsuku eziyi-7.Amagundane aphathwe nge-1, 2, 4, noma 8 mg/kg/day caspofungin, 1 mg/kg/day amphotericin B noma isilawuli semoto (amanzi acwecwe angenalutho).Ukusebenza kahle kwemodeli kwahlolwa ngezindlela ezintathu: ngokuqapha izinga lokusinda kwezilwane ze-10 eqenjini ngalinye lokwelapha, ngokuqapha umthwalo we-Candida ezinsweni nasezicubu zobuchopho zeqembu lesibili lezilwane eziphathwayo, kanye nokuhlola umlando wezinso.Futhi ingqondo.Iqembu lesithathu lezilwane eziphathwayo.Amagundane agunyazwa ukuhogela umoya we-CO 2 futhi akhuliswa emahoreni angu-30 (ukulawula okulashwe imoto kuphela) nangosuku lwesi-5 (amahora angu-24 ngemva komthamo wesi-4), 8 (amahora angu-24 ngemva komthamo wokugcina), kanye ne-14, amahora angu-21 kanye ne-histological. isampula yezicubu.(Ukwelashwa kwe-caspofungin kuphela), kanye nama-28 ngemuva kokuhlasela. |
Izithenjwa | [1].Mojumder DK, et al.Ukuhlola ubuthi be-retina be-intravitreal caspofungin esweni legundane.Tshala imali ye-Ophthalmol Vis Sci.2010 Nov;51(11):5796-803. [2].Flattery, Amy M. et al.Ukusebenza kwe-caspofungin kumodeli yegundane yentsha ye-central nervous system candidiasis.Ama-Antimicrobial Agents kanye ne-Chemotherapy (2011), 55 (7), 3491-3497. |
Izakhiwo zamakhemikhali nezomzimba ze-caspofungin acetate
Iphuzu elibilayo | 1408.1ºC ku-760 mmHg |
Ifomula yamangqamuzana | I-C56H96N10O19 |
Isisindo samangqamuzana | 1093.31000 |
Ikhwalithi enembile | 1092.64000 |
I-PSA | 412.03000 |
I-LogP | 0.06150 |
Izici zokubukeka | okumhlophe kuya ku-beige |
Umfutho we-vapor | 0mmHg ku-25°C |
Izimo zokugcina | 20°C |
Ukuncibilika kwamanzi | I-H2O: i-soluble15mg/mL (isixazululo esicacile) |
I-Caspofungin Acetate Customs
Ikhodi yangokwezifiso | 2933990099 |
Uhlolojikelele lwesiShayina | 2933990099. Amanye ama-heterocyclic compounds aqukethe kuphela i-nitrogen heteroatom.Izinga lentela elengeziwe: 17.0%.Isilinganiso sesaphulelo sentela: 13.0%.Izimo zokulawula: Akukho.Izindleko zezwe ezithandwa kakhulu: 6.5%.Intengo ejwayelekile: 20.0% |
Izici zesimemezelo | Igama lomkhiqizo, okuqukethwe kwesithako, ukusetshenziswa, i-hexamethylene chloride, sicela ubonise ukubukeka, i-6-caprolactam, sicela ubonise ukubukeka, usuku lokusayina |
Isifinyezo | 2933990090. izinhlanganisela ze-heterocyclic ezine-nitrogen hetero-athomu kuphela.I-VAT:17.0%.Izinga lesaphulelo sentela:13.0%..Intengo ye-MFN:6.5%.Intengo ejwayelekile:20.0% |
Inqubo Yokukhiqiza
I-Caspofungin idinga ukulungiswa ngobuchwepheshe bokuvutshelwa kwe-semi-synthetic.Umkhiqizo ongahluziwe wendandatho eyinhloko udinga ukutholwa ngobuchwepheshe bokuvutshelwa, bese umkhiqizo ophakathi nendawo utholakala ngokuhlukaniswa nokuhlanzwa, bese umkhiqizo ophakathi usetshenziswa njengento yokuqala ukuqedela ukuhlanganisa iketango elisemaceleni kusetshenziswa ubuchwepheshe bokwenziwa ukuze ekugcineni kutholwe. i-element eqondiwe.Ngenxa yokuthi imikhiqizo "ebilisiwe ye-semi-synthetic" idinga ukudlula izixhumanisi zobuchwepheshe eziningi njengokuvutshelwa, ukuhlukaniswa nokuhlanzwa, ukuhlanganiswa, njll., umzila wobuchwepheshe nokulawula ipharamitha yenqubo kuyinkimbinkimbi kakhulu ku-Chemicalbook.Ngaphezu kwalokho, izidingo zokulawula zokubhaliswa kwe-caspofungin, umkhiqizo ovutshiwe we-semi-synthetic, nazo ziphakeme kakhulu.Amadokhumenti okufaka isicelo adinga ukuqala emthonjeni wokuvutshelwa, hhayi kuphela ukuze atadishe ngokuhlelekile ukutshalwa kohlobo oluthile, ubuchwepheshe bokuvutshelwa, nobuchwepheshe bokuhlanza, kodwa futhi ukuhlola inqubo yokuhlanganisa.Umzila, izimo, nokulawulwa kokungcola kule nqubo, ngenxa yokuthi umkhiqizo wokugcina untekenteke impela, noma yikuphi ukunganaki kuzosula yonke imizamo yangaphambili, futhi ubunzima bobuchwepheshe nezindleko akuzona ezincane.
Kungenxa yokuthi kungenxa yezithiyo zobuchwepheshe eziphakeme kanye nesimo esihle sokuncintisana okwenza i-Hengrui Caspofungin igcine indawo enamanani entengo enhle uma kuqhathaniswa ngemva kokufakwa kuhlu kwayo.
Ukuvikelwa kwelungelo lobunikazi kuphelelwe yisikhathi ngo-2014
Ukuthengiswa kwemijovo ye-terminal caspofungin ezikhungweni zezokwelapha zomphakathi e-China (iyunithi: amayuan ayizinkulungwane eziyishumi)
Kuze kube manje, yimithi ejwayelekile kuphela ye-Hengrui Pharmaceuticals, i-Chia Tai Tianqing, i-Borui Pharmaceuticals, ne-Haisco egunyaziwe ukuthi ifakwe ohlwini.Imithi ye-Huadong?
Inkampani yokuqala yocwaningo ye-caspofungin acetate yi-Merck, futhi izicelo ezifakwe ohlwini zezinkampani eziyisi-6 ziyabuyekezwa futhi zivunyelwe, okuyi-Qilu Pharmaceutical, Nanjing Yinxing Pharmaceutical, Sihuan Pharmaceutical, Osaikang Pharmaceutical, Sino-US Huadong Pharmaceutical, kanye ne-Tian Weitical Bio.
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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...
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