ʻO Caspofungin Acetate Biological Activity
E wehewehe | ʻO ka Caspofungin Acetate kahi lāʻau antifungal hiki ke pale i ka synthesis o 1,3-β-d glucan synthase. |
Piliwaeʻano | ala hōʻailona >> Anti-infective >> Fungus Nā wahi noiʻi >> Infect |
I loko o vivonoiʻi | ʻO nāʻiole i hoʻokomoʻia me ka caspofunginʻaʻole i loaʻa i nā loli koʻikoʻi i kā lākou nalu ERG ma kahi hoʻonui vitreous o 0.41 a 4.1 μM, aʻaʻole i loaʻa i kā lākou retina nā loli morphological a iʻole ka nalowale pūnaewele.Ma ka vitreous concentration o 41 μM, ua hoʻemi ka caspofungin i ka amplitude o ka nalu, b a me ka pane paepae scotopic o ERG, a ua hoʻemi hoʻi i ka helu o nā cell i ka papa ganglion cell [1].Carprofungin (8 mg/kg) a i ʻole amphotericin B 1 mg/kg, intraperitoneal injection hoʻokahi manawa i ka lā 30 h ma hope o ka maʻi no 7 mau lā, pili i ka mālama kaʻa, 100% ola i ka lā 28, e hopena i ka lā 100% ka nui o ka make 11 , ma hope o ka hoʻopiʻi maʻi.Ke hoʻohālikelike ʻia me ka mālama kaʻa kaʻa i ka lā 5, ua hōʻemi ka caspofungin i ka hoʻihoʻi ʻana o Candida ola i loko o ka ʻōpū a me ka ʻiʻo lolo i ka wā i hiki ai ka ukana mana i kona piko.ʻO nā ʻiole i mālama ʻia me ka caspofungin ma kahi ʻano o 2 mg/kg a ʻoi aku paha ka haʻahaʻa haʻahaʻa o ka lolo i ka lā 5 ma mua o nā ʻiole i mālama ʻia me ka amphotericin B. ʻO ka Amphotericin B a me ka mālama ʻana i ka caspofungin ua hoʻemi ʻia ke kaumaha fungal renal e 1.7 log CFU/g a me 2.46 a 3.64 log CFU. /g, kēlā me kēia [2]. |
Holoholonahoʻokolohua | Ua hoʻomaka ʻia ka lāʻau antifungal ma hope o 30 mau hola ma hope o ka paʻakikī infectious a hāʻawi ʻia e intraperitoneal (ip) injection hoʻokahi i ka lā no 7 mau lā.Ua mālama ʻia nā ʻiole me ka 1, 2, 4, a i ʻole 8 mg / kg / lā caspofungin, 1 mg / kg / lā amphotericin B a i ʻole ka hoʻokele kaʻa (wai distilled sterile).Ua loiloi ʻia ka maikaʻi o ke kŘkohu ma nā ʻano ʻekolu: ma ka nānā ʻana i ke ola o nā holoholona he 10 i kēlā me kēia pūʻulu lapaʻau, ma ka nānā ʻana i ka ukana Candida i loko o ka puʻupaʻa a me ka lolo o ka lua o nā holoholona i mālama ʻia, a me ka loiloi histologically i nā puʻupaʻa.A lolo.ʻO ka hui ʻekolu o nā holoholona i mālama ʻia.Hoʻopau ʻia nā ʻiole e ka inhalation CO 2 a mālama ʻia i nā hola 30 (ka mālama kaʻa wale nō) a ma ka lā 5 (24 mau hola ma hope o ka 4th dose), 8 (24 mau hola ma hope o ka hopena hope loa), a me 14, 21 hola And histological. laʻana ʻiʻo.(ʻO ka lapaʻau caspofungin wale nō), a me 28 ma hope o ka hoʻouka ʻana. |
Nā kuhikuhi | [1].Mojumder DK, et al.Ka loiloi ʻana i ka ʻawaʻawa retinal o intravitreal caspofungin i ka maka ʻiole.Hoʻokomo i ka Ophthalmol Vis Sci.2010 Nov;51(11):5796-803. [2].Pāhili, Amy M. et al.ʻO ka maikaʻi o ka caspofungin i loko o kahi kiʻi ʻiole ʻōpio o ka candidiasis ʻōnaehana kūloko.Antimicrobial Agents and Chemotherapy (2011), 55 (7), 3491-3497. |
Nā waiwai kino a me ke kino o ka caspofungin acetate
Lae paila | 1408.1ºC ma 760 mmHg |
ʻAno molekala | C56H96N10O19 |
Kaumaha molekula | 1093.31000 |
ʻO ka maikaʻi pololei | 1092.64000 |
PSA | 412.03000 |
LogP | 0.06150 |
Nā hiʻohiʻona hiʻohiʻona | keʻokeʻo i ka beige |
Pumi mahu | 0mmHg ma 25°C |
Nā kūlana mālama | 20°C |
Ka hoʻoheheʻe wai | H2O: hiki ke hoʻoheheʻe ʻia 15mg/mL |
ʻO nā dute Caspofungin Acetate
Code dute | 2933990099 |
Nānā Kūlana Pākē | 2933990099. Nā pūhui heterocyclic ʻē aʻe i loaʻa nā heteroatoms nitrogen wale nō.Laki ʻauhau hoʻohui waiwai: 17.0%.Laki ʻauhau: 13.0%.Nā kūlana hoʻoponopono: ʻAʻohe.ʻO ka uku o ka lāhui i makemake nui ʻia: 6.5%.Ka uku nui: 20.0% |
Nā mea hoʻolaha | ʻO ka inoa o ka huahana, ka mea hoʻohui, hoʻohana, hexamethylene chloride, e ʻoluʻolu e hōʻike i ke ʻano, 6-caprolactam, e ʻoluʻolu e hōʻike i ke ʻano, ka lā kau inoa. |
Hōʻuluʻulu manaʻo | 2933990090. nā pūhui heterocyclic me (s) nitrogen hetero-atom wale nō.VAT:17.0%.Laki ʻauhau: 13.0%..Ka uku MFN: 6.5%.Ka uku nui: 20.0% |
Kaʻina Hana Hana
Pono e hoʻomākaukau ʻia ʻo Caspofungin e ka ʻenehana semi-synthetic fermentation.Pono e kiʻi ʻia ka huahana crude o ke apo nui ma o ka ʻenehana fermentation, a laila loaʻa ka huahana waena ma o ka hoʻokaʻawale ʻana a me ka hoʻomaʻemaʻe ʻana, a laila hoʻohana ʻia ka huahana waena e like me ka mea hoʻomaka e hoʻopau i ke kaulahao ʻaoʻao me ka hoʻohana ʻana i ka ʻenehana synthetic e loaʻa hope loa. ka Element target.No ka mea, pono e hele nā huahana "fermented semi-synthetic" i nā loulou ʻenehana he nui e like me ka fermentation, kaʻawale a me ka hoʻomaʻemaʻe, synthesis, etc.Eia kekahi, kiʻekiʻe loa nā koi hoʻoponopono no ka hoʻopaʻa inoa ʻana o ka caspofungin, kahi huahana semi-synthetic fermented.Pono nā palapala noi e hoʻomaka mai ke kumu fermentation, ʻaʻole wale no ka hoʻopaʻa pono ʻana i ka mahiʻai ʻana, ka ʻenehana fermentation, a me ka ʻenehana hoʻomaʻemaʻe, akā no ka ʻimi ʻana i ke kaʻina hana synthesis.ʻO ke ala, nā kūlana, a me ka mālama ʻana i nā haumia i ke kaʻina hana, no ka mea he palupalu ka huahana hope loa, ʻo ka mālama ʻole ʻana e hoʻopau i nā hana mua a pau, a ʻo ka pilikia ʻenehana a me ke kumukūʻai ʻaʻole ia he mea nui.
Ma muli o nā pale ʻenehana kiʻekiʻe a me kahi ʻāina hoʻokūkū maikaʻi i mālama ʻo Hengrui Caspofungin i kahi wahi kumu kūʻai maikaʻi ma hope o kāna papa inoa.
Ua pau ka pale patent i ka makahiki 2014
Ke kūʻai aku nei i nā ʻinikua caspofungin terminal ma nā keʻena olakino lehulehu ma Kina (ʻāpana: ʻumi tausani yuan)
A hiki i kēia manawa, ʻo nā lāʻau lapaʻau maʻamau o Hengrui Pharmaceuticals, Chia Tai Tianqing, Borui Pharmaceuticals, a me Haisco i ʻae ʻia no ka papa inoa.Huadong Medicine?
ʻO ka hui noiʻi mua o ka caspofungin acetate ʻo Merck, a ʻo ka papa inoa o nā hui 6 e nānā ʻia a ʻae ʻia, ʻo ia ʻo Qilu Pharmaceutical, Nanjing Yinxing Pharmaceutical, Sihuan Pharmaceutical, Osaikang Pharmaceutical, Sino-US Huadong Pharmaceutical, a me Tian Wei Biopharmaceuticals.
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NA POMAIKAI ANA IA
●Kiʻekiʻe Pressure Catalytic Hydrogenation.ʻO ke kiʻekiʻe o ka Hydrogenolysis Reaction.Cryogenic Reaction (<-78%C)
●Aromatic Heterocyclic Synthesis
● Hoʻoponopono hou
●Chiral Resolution
●Heck, Suzuki, Negishi, Sonogashira .Pane ʻo Gignard
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