Entecavir USP Yanduye B; Imfashanyo098045; Imfashanyo-098045; Etv; Enticavir; EntikaweiPian;

Ibisobanuro bigufi:

Ibicuruzwa birambuye

Ibicuruzwa

Gusaba

Entecavir （SQ 34676;BMS 200475） ihitamo kandi ikora HBV Inhibitor.Muri HepG2 selile EC50 agaciro ni 3.75 nM.Imiti igabanya ubukana bwa hepatite B n'imiti igabanya ubukana bwa mbere.

Ingaruka ya Entecavir

Iki gicuruzwa nikigereranyo cya guanine nucleoside, kigira ingaruka mbi kuri virusi ya hepatite B (HBV) polymerase.Irashobora kuba fosifora muri triphosifate ikora, kandi igice cya kabiri cyubuzima bwa triphosifate mungirangingo ni amasaha 15.Muguhangana na HBV polymerase isanzwe ya substrate deoxyguanosine triphosphate, entecavir triphosphate irashobora guhagarika ibikorwa byose uko ari bitatu bya virusi polymerase (reverse transcriptase): (1) Gutangiza polymerase ya HBV;(2) pregenomic mRNA Imiterere yumurongo mubi wo kwandukura inyandiko;(3) Synthesis yumurongo mwiza wa ADN ya HBV.Guhagarika inhibitori (Ki) ya entecavir triphosphate kuri HBV ADN polymerase ni 0.0012μM.Entecavir triphosphate igira ingaruka mbi zo guhagarika ingirabuzimafatizo α, β, δ ADN polymerase na mitochondrial γ ADN polymerase, ifite agaciro ka 18 kugeza 160 μM.

Ibipimo

Sobanura	Entecavir （SQ 34676;BMS 200475） iratoranya kandi ikora HBV Inhibitor。Muri selile HepG2 EC50 agaciro ni 3.75 nM.
Bifitanye isanoibyiciro	inzira yerekana ibimenyetso >> Kurwanya kwandura >> HBV Ahantu ubushakashatsi >> Yanduye
Intego	EC50: 3.75 nM (anti-HBV, selile HepG2) [2]
Muri vitroubushakashatsi	EC50 ya BMS-200475 kugeza HBV ni 3.75 nM.Yinjijwe muri primaire ya HBV, hanyuma intambwe yo gutangiza reaction transcriptase irabujijwe.Igikorwa cya virusi ya BMS-200475 kiri hasi cyane ugereranije nizindi virusi za RNA na ADN [1].Ugereranije nibindi bigereranya deoxyguanosine (penciclovir, ganciclovir, lobucavir na acyclovir) cyangwa lamivudine, entecavir irashobora kuba fosifori na metabolite ikora.Igice cya kabiri cyubuzima bwa Entecavir ni amasaha 15 [2].
Muri vivoubushakashatsi	BMS-200475 ivurwa mu kanwa buri munsi ikoresheje urugero ruri hagati ya 0,02 na 0.5 mg / kg uburemere bwumubiri mu gihe cyamezi 1 kugeza kuri 3, ibyo bikaba bishobora kugabanya neza urugero rwa virusi ya hepatite virusi (WHV) virusi yibiti byanduye bikabije [3].
Akagariigerageza	BMS 200475 itegurwa muri saline ya fosifate (PBS) hanyuma ikavangwa nuburyo bukwiye burimo 2% ya serumu y'inda.HepG2 2.2.15 ingemwe zatewe ku isahani 12 yuzuye ya Biocoat ya kolagen yometse ku isahani ya 5 × 10 5 ku iriba, ikabikwa mu masangano iminsi 2 kugeza kuri 3, hanyuma igapfundikirwa na mL 1 ya BMS 200475 giciriritse.Umubare wa HBV wakozwe ku munsi wa 10 [1].
Reba	[1].Innaimo SF, n'abandi.Kumenyekanisha BMS-200475 nkumuti ukomeye kandi uhitamo virusi ya hepatite B.Imiti igabanya ubukana.1997 Nyakanga; 41 (7): 1444-9. [2]Rivkin A, n'abandi.Isubiramo rya entecavir mukuvura indwara zidakira ya hepatite B.Inzira Med Res Opin.2005 Ugushyingo; 21 (11): 1845-57. [3]Genovesi EV, n'abandi.Ingaruka za karbocyclic 2'-deoxyguanosine nucleoside BMS-200475 muburyo bwibiti byanduye virusi ya hepatite B.Imiti igabanya ubukana.1998 Ukuboza; 42 (12): 3209-18.

Imiterere yumubiri na chimique ya Entecavir

Ubucucike	1.8 ± 0.1 g / cm³
Ingingo yo guteka	734.2ºC kuri 760 mmHg
Ingingo yo gushonga	249-252ºC
Inzira ya molekulari	C12H15N5O3
Uburemere bwa molekile	277.279
Ingingo ya Flash	397.9ºC
Ubwiza	277.117493
PSA	130.05000
LogP	-0.96
Ibiranga isura	Ifu yera-yera / ifu ya kristaline
Ironderero	1.837
Imiterere yo kubika	-20 ° C Ikonjesha

Gasutamo ya Entecavir

Kode ya gasutamo	2933990099
Incamake y'Ubushinwa	2933990099. Ibindi bikoresho bya heterocyclic birimo azote ya azote gusa.Igipimo cy'umusoro ku nyongeragaciro: 17.0%.Igipimo cyo kugabanyirizwa imisoro: 13.0%.Ibisabwa: Nta na kimwe.Igiciro cyigihugu gikunzwe cyane: 6.5%.Igiciro rusange: 20.0%
Ibimenyesha	Izina ryibicuruzwa, ibiyigize, koresha, hexamethylene chloride, nyamuneka werekane isura, 6-caprolactam, nyamuneka werekane isura, itariki yo gusinya
Incamake	2933990090. ibice bya heterocyclic hamwe na azote hetero-atom (s) gusa.TVA: 17.0%.Igipimo cyo kugabanyirizwa imisoro: 13.0%..Igiciro cya MFN: 6.5%.Igiciro rusange: 20.0%

Andi makuru:

Qu Qiang (PhD muri farumasi y’ubuvuzi, Ishami rya Farumasi, Ibitaro bya Xiangya, Kaminuza Nkuru y’Amajyepfo) na Wang Ruoguang (Umuganga w’Ubuvuzi, impamyabumenyi y'ikirenga muri biologiya, Ikigo cy’ubushakashatsi cy’ubuvuzi cya Changsha Ruoguang) na bo banditse ko: muri gahunda ya entecavir, entecavir ishobora gufatwa imyaka myinshi cyangwa imyaka 10.Kurenza imyaka.Kandi irashobora gukoreshwa nabagore batwite, ikerekana umutekano mwiza.

Urebye kuri ubwo buryo buzwi bwa farumasi ya farumasi, Entecavir irashobora kugira ingaruka nini ya virusi ya virusi, ntabwo ikora neza kuri HBV.

Dukunze kandi gukoresha Entecavir kugirango tuvure indwara zandurira mu myanya y'ubuhumekero ku ivuriro, kandi ingaruka ziratangaje.

Kugeza ubu, mu isesengura ryihuse ry’abarwayi barenga 500 COVID19 i Hubei (ahantu), umuntu umwe gusa ni we wafashe entecavir.Igihe cyo kwandikirwa cyari mu ntangiriro za Mutarama, hanyuma ibiyobyabwenge birahagarara.

Mugihe utera inkunga abaganga i Hubei, abaganga bamwe bo mu nzego z'ibanze, cyangwa amatsinda afite ibyago byinshi, kuri ubu bakoresha Entecavir mu gukumira COVID19, nta kibazo cyanduye.Abantu bakekwa gufata entecavir, ntamuntu wigeze atera imbere ngo asuzumwe na COVID19.

Ibibazo by'ipatanti:

Hariho inzira ebyiri, inzira 06 na 89 inzira.Iherezo rya patenti kubikorwa 06 ni kare cyane (birangira muri 2023)!Nubwo ikiguzi cyibikorwa ari gito, ireme ni ryiza, kandi abakozi barashobora gukomera, inama zabo bwite: Kubihingwa byimiti, koresha inzira ya 06 kugirango utirata cyane;kubigo bikorerwamo ibya farumasi, ntugafate fluke kandi ntugire ibyago byinshi.

Muri 2014, Chia Tai Tianqing yageze ku mwaka kugurisha miriyari 10 z'amadorari yishingikirije ku biyobyabwenge rusange nka entecavir, muri byo entecavir ikaba yari 20%.

Kuva entecavir yemerewe gutumizwa mu 2005, amasosiyete arenga 100 y’imiti yo mu gihugu yasabye kwandikisha ibicuruzwa;muri byo, amasosiyete yemewe yemewe arimo Jiangsu Zhengda Tianqing Pharmaceutical (yigana bwa mbere), Pharmaceutical ya Hainan Zhonghe, na Pharmaceutical Co., Fujian Guangxi Pharmaceutical Co., Ltd. Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Ibinyabuzima.

Imiti, Anhui Baker Biopharmaceutical, Uruganda rwa Farumasi ya Hunan Concord, Uruganda rukora imiti rwa Beijing Xiehe, Imiti ya Beijing Baiao, Pharmaceutical Xinlitai, Dongyangguang, nibindi.;kure guhera umunsi amasezerano yagenwe, iki gicuruzwa cyinjiye murwego rwamoko yatangajwe kuva 2007.

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● Synthesis ya Aromatic Heterocyclic
Re reaction Kuvugurura
Res Igisubizo cya Chiral
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