Entecavir USP poke B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir USP poke B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir（SQ 34676;Ko te BMS 200475） he Kaitiaki HBV whiriwhiri me te whai hua.I roto i nga pūtau HepG2 EC50 uara ko 3.75 nM.Ko nga rongoa hou mo te mate pukupuku B me te AIDS mo te rarangi tuatahi.
Te hua o te entecavir
Ko tenei hua he tairitenga guanine nucleoside, he awe te aukati i te mate hepatitis B (HBV) polymerase.Ka taea te phosphorylated ki triphosphate kaha, me te hawhe-ora o te triphosphate i roto i te pūtau he 15 haora.Ma te whakataetae me te deoxyguanosine triphosphate o te HBV polymerase, ka taea e te entecavir triphosphate te aukati i nga mahi e toru o te polymerase viral (whakamuri transcriptase): (1) HBV polymerase initiation;(2) pregenomic mRNA Te hanganga o te whenu kino o te whakawhitinga whakamuri;(3) Te whakahiato o te whenu pai o te HBV DNA.Ko te taumau aukati (Ki) o te entecavir triphosphate i runga i te HBV DNA polymerase he 0.0012μM.Ko te Entecavir triphosphate he kaha aukati ngoikore ki te pūtau α, β, δ DNA polymerase me te mitochondrial γ DNA polymerase, me te uara Ki o 18 ki te 160 μM.
| Whakaahuatia | Entecavir（SQ 34676;Ko te BMS 200475）he HBV Inhibitor whiriwhiri me te whai hua.I roto i nga pūtau HepG2 EC50 te uara 3.75 nM. |
| E pa anangā kāwai | ara tohu >> Anti-infective >> HBV Research areas >> Infect |
| Whainga | EC50: 3.75 nM (anti-HBV, pūtau HepG2)[2] |
| In vitrorangahau | Ko te EC50 o BMS-200475 ki te HBV he 3.75 nM.Ka whakauruhia ki roto i nga papaariki pūmua HBV, katahi ka aukatihia te taahiraa o te transcriptase whakamuri.Ko te mahi antiviral o BMS-200475 he tino iti ake i era atu huaketo RNA me te DNA [1].Ka whakatauritea ki etahi atu taarite deoxyguanosine (penciclovir, ganciclovir, lobucavir me te acyclovir) me te lamivudine ranei, ka kaha ake te phosphorylated entecavir ki tana metabolite kaha.Ko te haurua o te ora o Entecavir he 15 haora [2]. |
| I roto i te vivorangahau | Ko te BMS-200475 ka tukuna ma te waha i ia ra me te horopeta mai i te 0.02 ki te 0.5 mg/kg te taumaha o te tinana mo te 1 ki te 3 marama, ka taea te whakaiti i te taumata o te viremia woodchuck hepatitis virus (WHV) i roto i nga woodchucks pangia roa [3]. |
| Pūtauwhakamātau | Kua whakaritea te BMS 200475 i roto i te phosphate buffered saline (PBS) me te waimeha ki te reo e tika ana kei roto te 2% serum bovine fetal.HepG2 2.2.15 i ruia ki runga i te 12-puna Biocoat collagen-coat plate i te kiato o te 5x10 5 pūtau mo ia puna, ka pupuri i roto i te ahua whakakotahi mo te 2 ki te 3 ra, katahi ka kapi ki te 1 mL o BMS 200475 reo .I mahia te inenga HBV i te 10 o nga ra [1]. |
| Tohutoro | [1].Innaimo SF, et al.Ko te tautuhi i te BMS-200475 hei aukati kaha me te whiriwhiri mo te huaketo hepatitis B.Antimicrob Agents Chemother.1997 Hurae;41(7):1444-9.[2].Rivkin A, et al.He arotake o te entecavir i roto i te maimoatanga o te mate hepatitis B mau tonu.Curr Med Res Opin.2005 Noema;21(11):1845-57.[3].Genovesi EV, et al.Te kaha o te carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 i roto i te tauira woodchuck o te mate huaketo hepatitis B.Antimicrob Agents Chemother.1998 Hakihea;42(12):3209-18. |
Nga ahuatanga o te tinana me te matū o Entecavir
| Kiato | 1.8±0.1 g/cm3 |
| Kohuatanga | 734.2ºC i te 760 mmHg |
| Te rewa | 249-252ºC |
| tātai rāpoi ngota | C12H15N5O3 |
| Te taumaha ngota | 277.279 |
| Kohikohiko | 397.9ºC |
| Te kounga tika | 277.117493 |
| PSA | 130.05000 |
| RangitakiP | -0.96 |
| Nga ahuatanga o te ahua | He ma ki te ma-ma-ma/te kowhai te paura tioata |
| Taupū Refactive | 1.837 |
| Nga tikanga rokiroki | -20°C Te pouaka tio |
Tikanga Entecavir
| Waehere ritenga | 2933990099 |
| Tirohanga Hainamana | 2933990099. Ētahi atu pūhui heterocyclic kei roto anake nga heteroatom hauota.Te utu taake utu taapiri: 17.0%.Te utu utu taake: 13.0%.Nga tikanga whakahaere: Karekau.Te utu mo te motu tino pai: 6.5%.Te utu nui: 20.0% |
| Huānga Whakapuakanga | Ingoa hua, ihirangi whakauru, whakamahi, hexamethylene chloride, tohuhia te ahua, 6-caprolactam, tohuhia te ahua, te ra hainatanga |
| Whakarāpopototanga | 2933990090. pūhui heterocyclic me te hauota hetero-ngota anake.VAT:17.0%.Te utu utu taake:13.0%..Te utu MFN: 6.5%.Te utu nui:20.0% |
He korero taapiri:
Qu Qiang (PhD i roto i te rongoā haumanu, Tari o Pharmacy, Xiangya Hospital, Central South University) me Wang Ruoguang (Doctor of Medicine, postdoctoral i roto i te koiora, Changsha Ruoguang Medical Research Center) i tuhi ano: i roto i te tikanga entecavir, ka taea te tango entecavir mo etahi tau, mo te 10 tau ranei.Neke atu i nga tau.A ka taea e nga wahine hapu te whakamahi, e whakaatu ana i te haumaru pai.
Ma te whakatau mai i enei tikanga rongoa rongoa mole e mohiotia ana, tera pea ka whai hua a Entecavir ki te whaanui-a-whaanui, ehara i te mea whai hua ki te HBV anake.
He maha nga wa ka whakamahia e matou te Entecavir ki te rongoa i nga mate rewharewha i roto i te whare haumanu, a he mea whakamiharo te paanga.
I tenei wa, i roto i te tirohanga whakamuri neke atu i te 500 nga turoro COVID19 i Hubei (he waahi), kotahi noa te tangata i tango i te entecavir.Ko te wa whakahaunga i te timatanga o Hanuere, katahi ka mutu te rongoa.
I a ia e tautoko ana i nga kaimahi rongoa i Hubei, etahi o nga taote o mua, o nga roopu morearea nui ranei, kei te whakamahi i te Entecavir hei aukati i te COVID19, kaore he keehi o te mate.Ko nga tangata e whakapaetia ana e tango ana i te entecavir, karekau he tangata i ahu whakamua ki te mate COVID19.
Nga take patent:
E rua nga tukanga, 06 te tukanga me te 89 te tukanga.Ko te paunga o te patent mo te tukanga 06 he moata rawa (ka pau i te 2023)!Ahakoa he iti te utu o te tukanga, he pai te ahua o te kounga, a ka taea e nga kaimahi te kaha, te tohutohu whaiaro: Mo nga tipu matū, whakamahia te tukanga 06 kia kaua e whakahihi;mo nga kamupene rongoa, kaua e paopao, kaua hoki e tino morearea.
I te tau 2014, i eke a Chia Tai Tianqing ki nga hokonga a-tau mo te 10 piriona yuan ma te whakawhirinaki ki nga raau taero penei i te entecavir, ko te entecavir te 20%.
Mai i te wa i whakaaetia te entecavir mo te kawemai i te tau 2005, neke atu i te 100 nga kamupene rongoa a-whare kua tono mo te rehitatanga o te hua;i roto ia ratou, ko nga kamupene whakangao kua whakaaetia ko Jiangsu Zhengda Tianqing Pharmaceutical (whakarite tuatahi), Hainan Zhonghe Pharmaceutical, me Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Qingsong Pharmaceutical, Sichuan Haiscoutical 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, etc.;atu i te ra o te kirimana, kua uru tenei hua ki nga rarangi o nga momo rongonui rongonui mai i te tau 2007.
JIN DUN Medical kuaKo te tohu ISO me te whakatutuki i nga paerewa whakaputa GMP, e mahi ana i nga tohunga whakahiato raau taero o roto me tawahi me te whai wheako nui hei arahi i te R&D a te kamupene.
TE WHAKAMAHI OGY
●High Pressure Catalytic Hydrogenation .Tauhohenga Hydrogenolysis High Pressure.Tauhohenga Cryogenic (<-78%C)
●Hangai Heterocyclic Aromatic
●Rearrangement Reaction
●Tauira Hira
●Heck, Suzuki,Negishi,Sonogashira .Tauhohenga Gignard
Nga taputapu
He maha nga taputapu whakamatautau me te whakamatautau, penei i te: NMR (Bruker 400M) 、HPLC, chiral-HPLC, LC-MS, LC-MS/MS (API 4000), IR, UV, GC, GC-MS, Chromatography, Te Ngaruiti Ngaruiti, Te Whakarara Whakarara, Te Waahanga Matawai Rereke (DSC), Te Kaitiaki Irahiko...
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Kua awhinahia e matou etahi kamupene rongoa o roto, penei iHansoh, Hengrui me HEC Pharm.I konei ka whakaatuhia e matou tetahi waahanga o ratou.
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