Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir USP Ukungcola B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir (SQ 34676;I-BMS 200475) yi-HBV Inhibitor ekhethiweyo kwaye esebenzayo.Kwiiseli ze-HepG2 ixabiso le-EC50 yi-3.75 nM.Amachiza amva nje e-anti-hepatitis B kunye ne-anti-AIDS kwinqanaba lokuqala.
Isiphumo se-Entecavir
Le mveliso i-guanine nucleoside analog, enempembelelo yokuthintela kwi-virus ye-hepatitis B (HBV) polymerase.Inokuthi i-phosphorylated ibe yi-triphosphate esebenzayo, kunye nesiqingatha sobomi be-triphosphate kwiseli yiyure ezili-15.Ngokukhuphisana ne-HBV polymerase yendalo ye-substrate i-deoxyguanosine triphosphate, i-entecavir triphosphate inokuthintela yonke imisebenzi emithathu ye-polymerase ye-viral (reverse transcriptase): (1) i-HBV polymerase initiation;(2) i-pregenomic mRNA Ukuqulunqwa komtya ombi wokuguqulela umva;(3) Ukwenziwa komcu ovumayo we-HBV DNA.I-inhibitory constant (Ki) ye-entecavir triphosphate kwi-HBV DNA polymerase yi-0.0012μM.I-Entecavir triphosphate ine-inhibitory effect ebuthakathaka kwi-cell α, β, δ DNA polymerase kunye ne-mitochondrial γ DNA polymerase, kunye nexabiso le-Ki le-18 ukuya kwi-160 μM.
| Chaza | Entecavir (SQ 34676;I-BMS 200475) iyakhetha kwaye iyasebenza i-HBV Inhibitor.Kwi-HepG2 iiseli EC50 ixabiso yi-3.75 nM. |
| Eyeleleneyoiindidi | indlela yomqondiso >> Anti-intsholongwane >> Iindawo zophando HBV >> Yosulela |
| Ekujoliswe kuko | EC50: 3.75 nM (anti-HBV, HepG2 iseli)[2] |
| I-In vitroizifundo | I-EC50 ye-BMS-200475 ukuya kwi-HBV yi-3.75 nM.Ifakwe kwi-HBV protein primers, kwaye emva koko inyathelo lokuqala le-reverse transcriptase liyathintelwa.Umsebenzi we-antiviral we-BMS-200475 usezantsi kakhulu kunezinye iintsholongwane ze-RNA kunye ne-DNA [1].Xa kuthelekiswa namanye ama-analogs e-deoxyguanosine (i-penciclovir, i-ganciclovir, i-lobulavir kunye ne-acyclovir) okanye i-lamivudine, i-entecavir inokuthi ibe yi-phosphorylated kwi-metabolite yayo esebenzayo.I-intracellular half-life of Entecavir yi-15 iiyure [2]. |
| Kwi-vivouphando | I-BMS-200475 iphathwa ngomlomo imihla ngemihla kunye ne-dose ukusuka kwi-0.02 ukuya kwi-0.5 mg / kg ubunzima bomzimba kwi-1 ukuya kwiinyanga ze-3, ezinokunciphisa ngokufanelekileyo izinga le-woodchuck hepatitis virus (WHV) viremia kwi-woodchucks enesifo esingapheliyo [3]. |
| Iseliumfuniselo | I-BMS 200475 ilungiswa nge-phosphate buffered saline (PBS) yaze yaxutywa ngesiphakathi esifanelekileyo esiqulethe i-2% ye-fetus bovine serum.Iiseli ze-HepG2 ze-2.2.15 zifakwe kwi-12-well ye-Biocoat i-collagen-coated plate kubuninzi be-5 × 10 iiseli ze-5 kwiqula ngalinye, kwaye zigcinwe kwindawo edibeneyo iintsuku ezi-2 ukuya kwezi-3, kwaye zigqunywe nge-1 mL ye-BMS 200475. phakathi .Ubalo lwe-HBV lwenziwa ngomhla we-10 [1]. |
| Iimbekiselo | [1].Innaimo SF, et al.Ukuchongwa kwe-BMS-200475 njenge-inhibitor enamandla kwaye ekhethiweyo ye-virus ye-hepatitis B.Antimicrob Agents Chemother.1997 Jul;41(7):1444-9.[2].Rivkin A, et al.Ukuphononongwa kwe-entecavir kunyango lwe-hepatitis B engapheliyo.Curr Med Res Opin.2005 Nov;21(11):1845-57 [3].Genovesi EV, et al.Ukusebenza kwe-carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 kwimodeli ye-woodchuck ye-virus ye-hepatitis B.Antimicrob Agents Chemother.1998 Dec;42(12):3209-18. |
Iimpawu zomzimba kunye neekhemikhali ze-Entecavir
| Ukuxinana | 1.8±0.1 g/cm3 |
| Indawo yokubilisa | 734.2ºC ku-760 mmHg |
| Indawo yokunyibilika | 249-252ºC |
| Ifomula yemolekyuli | I-C12H15N5O3 |
| Ubunzima bemolekyuli | 277.279 |
| Indawo yokuflasha | 397.9ºC |
| Umgangatho ochanekileyo | 277.117493 |
| PSA | 130.05000 |
| LogP | -0.96 |
| Iimpawu zenkangeleko | Imhlophe ukuya kumhlophe-mhlophe / umgubo wekristale omthubi |
| Isalathiso sokuqhafaza | 1.837 |
| Iimeko zokugcina | -20°C Isikhenkcisi |
Entecavir Customs
| Ikhowudi yeCustoms | 2933990099 |
| Chinese Overview | 2933990099. Ezinye iikhompawundi ze-heterocyclic eziqukethe kuphela i-nitrogen heteroatoms.Ixabiso lerhafu eyongeziweyo: 17.0%.Izinga lesaphulelo serhafu: 13.0%.Imiqathango yolawulo: Akukho.Umrhumo wesizwe othandwa kakhulu: 6.5%.Uluhlu lweerhafu ngokubanzi: 20.0% |
| Iimpawu zesibhengezo | Igama lemveliso, umxholo wezithako, ukusetyenziswa, i-hexamethylene chloride, nceda ubonise imbonakalo, i-6-caprolactam, nceda ubonise imbonakalo, umhla wokusayina |
| Isishwankathelo | 2933990090. i-heterocyclic compounds kunye ne-nitrogen hetero-atom (s) kuphela.IVAT:17.0%.Ireyithi yesaphulelo serhafu:13.0%..Intlawulo yeMFN:6.5%.Uluhlu lweerhafu ngokubanzi: 20.0% |
Iinkcukacha ezongezelelweyo:
I-Qu Qiang (i-PhD kwi-pharmacology yekliniki, iSebe le-Pharmacy, iSibhedlele sase-Xiangya, iYunivesithi yaseMzantsi Afrika) kunye no-Wang Ruoguang (uGqirha wezoNyango, i-postdoctoral kwi-biology, i-Changsha Ruoguang Medical Research Centre) nayo yabhala ukuba: kwi-regimen ye-entecavir, i-entecavir inokuthathwa. iminyaka emininzi okanye iminyaka eyi-10.Ngaphezu kweminyaka.Kwaye inokusetyenziswa ngabasetyhini abakhulelweyo, ebonisa ukhuseleko oluhle.
Ukuqwalasela ezi ndlela zaziwayo ze-molecular pharmacological, i-Entecavir ingaba nefuthe elibanzi le-antiviral, elingasebenzi kuphela kwi-HBV.
Sisoloko sisebenzisa i-Entecavir ukunyanga izifo zentsholongwane yokuphefumula kwikliniki, kwaye umphumo uyamangalisa.
Okwangoku, kuhlalutyo lokubuyela emva kwezigulana ezingaphezu kwama-500 ze-COVID19 e-Hubei (indawo), ngumntu omnye kuphela owathatha i-entecavir.Ixesha elimiselweyo lalisekuqaleni kukaJanuwari, kwaye ke iyeza layekwa.
Ngelixa bexhasa abasebenzi bezonyango e-Hubei, abanye oogqirha abasezantsi, okanye amaqela asemngciphekweni omkhulu, ngoku asebenzisa i-Entecavir ukunqanda i-COVID19, akukho meko yosulelo.Abantu ekurhaneleka ukuba bathatha i-entecavir, akukho mntu uqhubele phambili wafunyaniswa ukuba une-COVID19.
Imiba yePatent:
Zimbini iinkqubo, 06 inkqubo kunye 89 inkqubo.Ukuphelelwa kwelungelo lomenzi wenkqubo ye-06 kusekude kakhulu (iphelelwa ngo-2023)!Nangona iindleko zenkqubo ziphantsi, umgangatho ulungile, kwaye abasebenzi banokuba namandla, iingcebiso zomntu: Kwizityalo zemichiza, sebenzisa inkqubo ye-06 ukuba ungabi nekratshi kakhulu;kwiinkampani ezixuba amayeza, musa ukuthatha i-fluke kwaye ungabi yingozi kakhulu.
Kwi-2014, i-Chia Tai Tianqing iphumelele kwiintengiso zonyaka ze-10 yezigidigidi ze-yuan ngokuthembela kumachiza aqhelekileyo afana ne-entecavir, apho i-entecavir ibalwa kwi-20%.
Ekubeni i-entecavir ivunyiwe ukuba ingeniswe kwi-2005, ngaphezu kweenkampani ze-100 zasekhaya zonyango ziye zafaka isicelo sokubhaliswa kwemveliso;phakathi kwabo, iinkampani zokuvelisa ezivunyiweyo ziquka i-Jiangsu Zhengda Tianqing Pharmaceutical (ukulinganisa kokuqala), i-Hainan Zhonghe Pharmaceutical, kunye ne-Fujian Guangxi Pharmaceutical Co., Ltd. I-Shengtang Pharmaceutical, i-Jiangxi Qingfeng Pharmaceutical, i-Suzhou Dawnrays Pharmaceutical Pharmaceutical, i-Shaingchung i-Qingfeng Pharmaceutical, i-Shaingchung. Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Biochemical.
Pharmaceutical, Anhui Baker Biopharmaceutical, Hunan Concord Pharmaceutical Industry, Beijing Xiehe Pharmaceutical Factory, Beijing Baiao Pharmaceutical, Xinlitai Pharmaceutical, Dongyangguang, njl.;ukusuka kumhla wekhontrakthi, le mveliso ingene kwiintlobo zeentlobo ezidumileyo ezichazwe ukususela ngo-2007.
JIN DUN Medical uyeIsiqinisekiso se-ISO kwaye sidibana nemigangatho yemveliso ye-GMP, kuqeshwe iingcali zasekhaya nezangaphandle zokwenziwa kweziyobisi ezinamava atyebileyo ukukhokela iR&D yenkampani.
I-TECHNOL OGY I-ADVANTAGES
●Uxinzelelo oluPhezulu lweCatalytic Hydrogenation.Uxinzelelo oluPhezulu lwe-Hydrogenolysis Reaction.I-Cryogenic Reaction (<-78%C)
● I-Aromatic Heterocyclic Synthesis
● Ukusabela ngokutsha
● IsiGqibo seChiral
●Heck, Suzuki,Negishi,Sonogashira .Giignard Reaction
Izixhobo
ILebhu yethu inezixhobo ezahlukeneyo zovavanyo kunye novavanyo, ezifana ne: 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, iKhalorimitha yokuSkena okwahlukileyo (DSC), iMicroscope ye-Electron...
R&D Iqela
I-Jindun Medical ineqela labasebenzi abaqeqeshiweyo be-R&D, kwaye iqeshe iingcali ezininzi zokwenziwa kweziyobisi zasekhaya nezangaphandle ukukhokela i-R&D, ukwenza udibaniso lwethu luchaneke ngakumbi kwaye lusebenze kakuhle.
Siye sanceda iinkampani ezininzi eziphezulu zamachiza zasekhaya, ezifanaHansoh, Hengrui kunye ne-HEC Pharm.Apha siza kubonisa inxalenye yazo.
Customization Case One:
Inombolo yeCas: 110351-94-5
Ityala leSibini:
Inombolo yeCas: 144848-24-8
Customization Case Three:
Inombolo yeCas: 200636-54-0
1.Lungiselela abaPhakathi abatsha okanye ii-APIs.Ngokufanayo nokwabelana ngetyala elingasentla, abathengi baneemfuno ze-Intermediates ezithile okanye ii-APIs, kwaye abanakuzifumana iimveliso ezifunekayo kwimarike, ngoko sinokunceda ukwenza ngokwezifiso.
2.Ukuphuculwa kweNkqubo yeeMveliso eziDala.Iqela lethu liya kunceda ukukhulisa nokuphucula imveliso enjalo indlela yokusabela indala, ixabiso lemveliso liphezulu, kwaye ukusebenza kakuhle kuphantsi.Sinokubonelela ngamaxwebhu apheleleyo okuhanjiswa kwetekhnoloji kunye nokuphuculwa kwenkqubo, sincede umthengi kwimveliso esebenzayo.
Ukusuka ekujoliswe kuko ngamachiza ukuya kwi-INDs, iJIN DUN Medical ikubonelelaisitophu esinye sezisombululo ze-R&D ezenzelwe wena.
I-JIN DUN Medical igxininisa ekudaleni iqela elinamaphupha, ukwenza iimveliso ezinesidima, ubuqili, ubukhali, kwaye uphume konke ukuze ube liqabane elithembekileyo kunye nomhlobo wabathengi!
![iCasp ungin acetate;Caspofungin acetate;Cancidas;Caspofungin acetate [USAN:BAN:JAN];](http://cdn.globalso.com/jindunchem-med/fbe17385-300x300.jpg)
![5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]- 5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2 (4h)-enye](http://cdn.globalso.com/jindunchem-med/image41-300x300.png)
![2-butyl-5-nitro-3-benzofuranyl) [4-[3-(dibutylaMino) propoxy]phenyl]](http://cdn.globalso.com/jindunchem-med/922e79ba.jpg)