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I-Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

I-Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;Isithombe Esifakiwe
  • I-Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

I-Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

Incazelo emfushane:


Imininingwane Yomkhiqizo

Omaka bomkhiqizo

Isicelo

I-Entecavir (SQ 34676;I-BMS 200475) iyi-HBV Inhibitor ekhethiwe futhi esebenzayo.Kumaseli e-HepG2 EC50 inani ngu-3.75 nM.Imithi yakamuva yokulwa nesifo sokusha kwesibindi kohlobo B kanye nemithi yokuqala yokulwa nengculazi.

Umphumela we-Entecavir

Lo mkhiqizo uyi-guanine nucleoside analog, enomphumela ovimbelayo ku-hepatitis B virus (HBV) polymerase.Ingenziwa i-phosphorylated ibe yi-triphosphate esebenzayo, kanti isigamu sempilo ye-triphosphate esitokisini singamahora ayi-15.Ngokuncintisana ne-HBV polymerase's natural substrate deoxyguanosine triphosphate, i-entecavir triphosphate ingavimbela yonke imisebenzi emithathu ye-viral polymerase (reverse transcriptase): (1) ukuqaliswa kwe-HBV polymerase;(2) i-pregenomic mRNA Ukwakheka kwe-negative strand yokulotshwa okuhlanekezelwe;(3) Ukuhlanganiswa komucu omuhle we-HBV DNA.I-inhibitory constant (Ki) ye-entecavir triphosphate ku-HBV DNA polymerase yi-0.0012μM.I-Entecavir triphosphate inomphumela obuthakathaka wokuvimbela kuseli α, β, δ DNA polymerase kanye ne-mitochondrial γ DNA polymerase, enenani le-Ki le-18 kuya ku-160 μM.

Amapharamitha

Chaza

 I-Entecavir (SQ 34676;I-BMS 200475) iyakhetha futhi iyasebenza i-HBV Inhibitor.Kumaseli e-HepG2 EC50 inani lingu-3.75 nM.

Okuhlobeneizigaba

 indlela yesignali >> Anti-infective >> Izindawo zocwaningo ze-HBV >> Thelela

Ithagethi

 EC50: 3.75 nM (anti-HBV, HepG2 cell)[2]

In vitroizifundo

 I-EC50 ye-BMS-200475 kuya ku-HBV ingu-3.75 nM.Ihlanganiswe ku-HBV protein primers, bese isinyathelo sokuqala se-reverse transcriptase siyavinjelwa.Umsebenzi we-antiviral we-BMS-200475 uphansi kakhulu kunamanye amagciwane e-RNA ne-DNA [1].Uma kuqhathaniswa namanye ama-analogues e-deoxyguanosine (i-penciclovir, i-ganciclovir, i-lobulavir ne-acyclovir) noma i-lamivudine, i-entecavir cishe i-phosphorylated ku-metabolite yayo esebenzayo.I-intracellular half-life ye-Entecavir ingamahora angu-15 [2].

Nge-vivoucwaningo

 I-BMS-200475 iphathwa ngomlomo nsuku zonke nge-dose kusuka ku-0.02 kuya ku-0.5 mg / kg isisindo somzimba wezinyanga ezingu-1 kuya kwezingu-3, ​​ezinganciphisa ngokuphumelelayo izinga le-woodchuck hepatitis virus (WHV) viremia ezikhungweni ze-woodchucks ezingapheli [3].

Iseliukuhlola

 I-BMS 200475 ilungiswa nge-phosphate buffered saline (PBS) futhi ixutshwe ngendawo efanele equkethe u-2% we-fetus serum.Amaseli e-HepG2 2.2.15 ahlwanyelwe epuleti elihlanganiswe ne-Biocoat-collagen-coat eline-12-coat ekumineni kwamaseli angu-5 × 10 5 emthonjeni ngamunye, futhi agcinwa esimweni sokuhlangana izinsuku ezingu-2 kuya kwezingu-3, ​​bese embozwa nge-1 mL ye-BMS 200475. okuphakathi .Ukulinganisa kwe-HBV kwenziwa ngosuku lwe-10 [1].

Izithenjwa

 [1].Innaimo SF, et al.Ukuhlonzwa kwe-BMS-200475 njenge-inhibitor enamandla futhi ekhethiwe yegciwane le-hepatitis B.Ama-Antimicrob Agents Chemother.1997 Jul;41(7):1444-9.[2].U-Rivkin A, et al.Ukubuyekezwa kwe-entecavir ekwelapheni ukutheleleka okungapheli kwe-hepatitis B.I-Curr Med Res Opin.2005 Nov;21(11):1845-57.[3].I-Genovesi EV, et al.Ukusebenza kwe-carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 kumodeli ye-woodchuck yokutheleleka ngegciwane le-hepatitis B.Ama-Antimicrob Agents Chemother.1998 Dec;42(12):3209-18.

Izakhiwo zomzimba nezamakhemikhali ze-Entecavir

Ukuminyana

 1.8±0.1 g/cm3

Iphuzu elibilayo

 734.2ºC ku-760 mmHg

Iphoyinti lokuncibilika

 249-252ºC

Ifomula yamangqamuzana

 I-C12H15N5O3

Isisindo samangqamuzana

 277.279

Iphoyinti le-Flash

 397.9ºC

Ikhwalithi enembile

 277.117493

I-PSA

 130.05000

I-LogP

 -0.96

Izici zokubukeka

 Impushana emhlophe ukuya kokumhlophe ukuya kokumhlophe/ophuzi

Inkomba ye-refractive

 1.837

Izimo zokugcina

 -20°C Isiqandisi

Entecavir 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%

Ulwazi Olwengeziwe:

I-Qu Qiang (i-PhD ku-pharmacology yomtholampilo, uMnyango Wekhemisi, Isibhedlela i-Xiangya, i-Central South University) no-Wang Ruoguang (Udokotela Wezokwelapha, i-postdoctoral in biology, i-Changsha Ruoguang Medical Research Centre) futhi wabhala ukuthi: ohlelweni lwe-entecavir, i-entecavir ingathathwa. iminyaka eminingana noma ngisho neminyaka eyi-10.Ngaphezu kweminyaka.Futhi ingasetshenziswa ngabesifazane abakhulelwe, ebonisa ukuphepha okuhle.

Uma sibheka lezi zinqubo ze-pharmacological ze-molecular, i-Entecavir ingase ibe nomphumela we-antiviral obanzi, hhayi kuphela osebenzayo ngokumelene ne-HBV.

Siphinde sisebenzise i-Entecavir ukuphatha izifo zokuphefumula ezibangelwa amagciwane emtholampilo, futhi umphumela uyamangalisa.

Njengamanje, ekuhlaziyeni okubuyayo kweziguli ezingaphezu kwama-500 ze-COVID19 e-Hubei (indawo), umuntu oyedwa kuphela owathatha i-entecavir.Isikhathi somuthi sasisekuqaleni kukaJanuwari, kwase kumiswe umuthi.

Ngenkathi besekela abasebenzi bezokwelapha e-Hubei, abanye odokotela basemazingeni aphansi, noma amaqembu asengozini enkulu, okwamanje asebenzisa i-Entecavir ukuvimbela i-COVID19, alikho icala lokutheleleka.Abantu okusolwa ukuthi bathatha i-entecavir, akekho osethuthukele ekutholakaleni ukuthi une-COVID19.

Izinkinga ze-patent:

Ikakhulukazi kunezinqubo ezimbili, inqubo ye-06 kanye nenqubo engama-89.Ukuphelelwa yisikhathi kwelungelo lobunikazi lenqubo ye-06 kusesekuseni kakhulu (kuphelelwa yisikhathi ngo-2023)!Nakuba izindleko zenqubo ziphansi, izinga lihle uma kuqhathaniswa, futhi izisebenzi zingaba iseluleko esiqinile, somuntu siqu: Ezitshalweni zamakhemikhali, sebenzisa inqubo 06 ukuze ungazikhukhumezi kakhulu;ezinkampanini ezithaka imithi, ungathathi i-fluke futhi ungabi yingozi kakhulu .

Ngo-2014, i-Chia Tai Tianqing yazuza ukuthengiswa konyaka kwe-yuan eyizigidi eziyizinkulungwane ezingu-10 ngokuthembela emithini ejwayelekile efana ne-entecavir, okuyi-entecavir ebalelwa ku-20%.

Njengoba i-entecavir ivunyelwe ukungenisa ku-2005, izinkampani ezingaphezu kwe-100 zemithi yasekhaya ziye zafaka isicelo sokubhaliswa komkhiqizo;phakathi kwazo, izinkampani zokukhiqiza ezigunyaziwe zifaka i-Jiangsu Zhengda Tianqing Pharmaceutical (ukulingisa kokuqala), i-Hainan Zhonghe Pharmaceutical, kanye ne-Fujian Guangxi Pharmaceutical Co., Ltd. I-Shengtang Pharmaceutical, i-Jiangxi Qingfeng Pharmaceutical, i-Suzhou Dawnrays Pharmaceutical, i-Shaingchung'ing Pharmaceutical, i-Singchuing Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Biochemical.

Ezemithi, Anhui Baker Biopharmaceutical, Hunan Concord Pharmaceutical Industry, Beijing Xiehe Pharmaceutical Factory, Beijing Baiao Pharmaceutical, Xinlitai Pharmaceutical, Dongyangguang, njll.;kusukela ngosuku lwenkontileka, lo mkhiqizo ungene ezinhlotsheni zezinhlobonhlobo ezimenyezelwe kusukela ngo-2007.

Ulayini Womkhiqizo Ohlanganisiwe Wezinsiza

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Isitifiketi

I-JIN DUN Medical ineIziqu ze-ISO futhi ihlangabezana namazinga okukhiqiza e-GMP, kuqashwe ochwepheshe basekhaya nabangaphandle abanolwazi olunzulu lokuqondisa i-R&D yenkampani.

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Izinzuzo Zokwenza Ngokwezifiso Kwezokwelapha

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

I-JIN DUN R&D

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

I-Jindun Medical ineqembu labasebenzi abangochwepheshe be-R&D, futhi isebenzisa ochwepheshe abaningi bokwenziwa kwezidakamizwa basekhaya nabangaphandle ukuze baqondise i-R&D, okwenza ukuhlanganiswa kwethu kunembe kakhudlwana futhi kusebenze kahle.

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Ukwabelana Kwamacala

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: 110351-94-5

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Ikesi Lokwenza Ngokwezifiso:

Inombolo yeCas: 144848-24-8

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Ikesi Lesithathu Lokwenza Ngokwezifiso:

Inombolo yeCas: 200636-54-0

Imodi Yokubambisana

1.Enza ngendlela oyifisayo i-New Intermediates noma ama-API.Ngokufanayo nokwabelana kwecala elingenhla, amakhasimende anezidingo ze-Intermediates ethile noma ama-API, futhi awakwazi ukuthola imikhiqizo edingekayo emakethe, lapho-ke singasiza Ukwenza Ngokwezifiso.

2.Ukuthuthukisa Inqubo Yemikhiqizo Emidala.Ithimba lethu lizosiza Ukuthuthukisa futhi lithuthukise ukukhiqiza okunjalo okuyindlela yokusabela endala, izindleko zokukhiqiza ziphezulu, nokusebenza kahle kuphansi.Singahlinzeka ngemibhalo egcwele yokudluliswa kobuchwepheshe kanye nokuthuthukiswa kwenqubo, sisize ikhasimende ngokukhiqiza okuphumelelayo.

Ukusuka kokuhlosiwe kwezidakamizwa kuye kuma-IND, i-JIN DUN Medical ikunikezaizixazululo zomuntu siqu ze-R&D zokuma okukodwa.

I-JIN DUN Medical iphikelela ekwakheni iqembu elinamaphupho, ukwenza imikhiqizo enesizotha, ecophelelayo, eqinile, futhi siphume konke ukuze sibe uzakwethu othembekile nomngane wamakhasimende!

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