Entecavir USP adịghị ọcha B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

Nkọwa dị mkpirikpi:

Nkọwa ngwaahịa

Mkpado ngwaahịa

Ngwa

Entecavir (SQ 34676;BMS 200475) bụ onye na-ahọrọ HBV Inhibitor ma dị irè.N'ime sel HepG2 EC50 uru bụ 3.75 nM.Ọgwụ mgbochi ịba ọcha n'anya B na ọgwụ mgbochi AIDS kacha ọhụrụ.

Mmetụta Entecavir

Ngwaahịa a bụ analọgụ guanine nucleoside, nke nwere mmetụta mgbochi na nje ịba ọcha n'anya B (HBV) polymerase.Enwere ike itinye ya na phosphorylate n'ime triphosphate na-arụ ọrụ, na ọkara ndụ nke triphosphate na cell bụ awa 15.Site n'iso HBV polymerase si eke mkpụrụ deoxyguanosine triphosphate, entecavir triphosphate nwere ike igbochi niile atọ omume nke viral polymerase (reverse transcriptase): (1) HBV polymerase mmalite;(2) pregenomic mRNA Nhazi nke eriri na-adịghị mma nke ntụgharị ntụgharị;(3) Njikọ nke eriri dị mma nke HBV DNA.Ihe mgbochi mgbe niile (Ki) nke entecavir triphosphate na HBV DNA polymerase bụ 0.0012μM.Entecavir triphosphate nwere mmetụta mgbochi na-adịghị ike na cell α, β, δ DNA polymerase na mitochondrial γ DNA polymerase, yana uru Ki nke 18 ruo 160 μM.

Oke

Kọwaa	Entecavir (SQ 34676;BMS 200475) bụ nhọrọ ma dị irè HBV Inhibitor. N'ime mkpụrụ ndụ HepG2 EC50 uru bụ 3.75 nM.
Ejikọtara yaedemede	Ụzọ mgbaàmà Malite >> Mgbochi na-efe efe >> HBV Research Mpaghara >> Ọrịa
Ebumnuche	EC50: 3.75 nM (mgbochi HBV, cell HepG2)[2]
In vitroọmụmụ	EC50 nke BMS-200475 ruo HBV bụ 3.75 nM.A na-etinye ya n'ime protein primers HBV, mgbe ahụ, a na-egbochi mmalite mmalite nke transcriptase.Ọrụ mgbochi nje nke BMS-200475 dị ala karịa nje RNA na DNA ndị ọzọ [1].E jiri ya tụnyere analogues deoxyguanosine ndị ọzọ (penciclovir, ganciclovir, lobucavir na acyclovir) ma ọ bụ lamivudine, entecavir nwere ike ịbụ phosphorylated na metabolite na-arụ ọrụ.Ọkara ndụ intracellular nke Entecavir bụ awa iri na ise [2].
Na vivonyocha	A na-agwọ BMS-200475 ọnụ kwa ụbọchị site na 0.02 ruo 0.5 mg / kg arọ ahụ maka ọnwa 1 ruo 3, nke nwere ike ibelata ọkwa nke nje ịba ọcha n'anya woodchuck (WHV) nke ọma na woodchucks na-adịghị ala ala [3].
Cellnnwale	A na-akwado BMS 200475 na saline buffered phosphate (PBS) wee gbarie ya na usoro kwesịrị ekwesị nke nwere serum bovine 2% nke nwa ebu n'afọ.A na-akụ mkpụrụ ndụ HepG2 2.2.15 na efere 12-nke ọma Biocoat collagen na njupụta nke sel 5 × 10 5 kwa nke ọma, ma debe ya na steeti confluent maka ụbọchị 2 ruo 3, wee kpuchie ya na 1 ml nke BMS 200475. ọkara .Emere ọnụọgụ HBV n'ụbọchị nke iri [1].
Ntụaka	[1].Innaimo SF, et al.Nchọpụta nke BMS-200475 dị ka onye na-egbochi nje ịba ọcha n'anya B dị ike na nhọrọ.Antimicrob Agents Chemother.1997 Jul; 41 (7): 1444-9 .[2].Rivkin A, et al.Nyochaa nke entecavir na ọgwụgwọ ọrịa ịba ọcha n'anya B na-adịghị ala ala.Curr Med Res Opin.2005 Nov; 21 (11): 1845-57 .[3].Genovesi EV, et al.Ịrụ ọrụ nke carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 na ụdị woodchuck nke ọrịa ịba ọcha n'anya B.Antimicrob Agents Chemother.1998 Dec; 42 (12): 3209-18 .

Njirimara anụ ahụ na kemịkalụ nke Entecavir

Njupụta	1.8±0.1 g/cm³
Ebe esi nri	734.2ºC na 760 mmHg
Ebe mgbaze	249-252ºC
Usoro ihe omimi	C12H15N5O3
Ibu arọ molekụla	277.279
ebe mgbari	397.9ºC
Ogo ziri ezi	277.117493
PSA	130.05000
LogP	-0.96
Àgwà mpụta	Uzuzu crystalline ọcha ruo na-acha ọcha/acha odo odo
Ntụgharị ntụgharị	1,837
Ọnọdụ nchekwa	-20°C friza

Ụlọ ọrụ Entecavir

Koodu kọstọm	2933990099
Nchịkọta ndị China	2933990099. Ogige heterocyclic ndị ọzọ nwere naanị nitrogen heteroatoms.Ọnụ ụtụ isi agbakwunyere ọnụ ahịa: 17.0%.Ọnụ ego nkwụghachi ụtụ: 13.0%.Ọnọdụ nchịkwa: Ọ dịghị.Tarifụ obodo kacha amasị ya: 6.5%.Tarifu izugbe: 20.0%
Ihe nkwupụta	Aha ngwaahịa, ihe eji eme ihe, ojiji, hexamethylene chloride, biko gosi ọdịdị ya, 6-caprolactam, biko gosi ọdịdị, ụbọchị nbinye aka.
Nchịkọta	2933990090. ogige heterocyclic na nitrogen hetero-atom (s) naanị.VAT: 17.0%.Ọnụ ego nkwụghachi ụtụ: 13.0%..Tarifụ MFN: 6.5%.Tarifu izugbe: 20.0%

Ozi Mgbakwunye:

Qu Qiang (PhD na ụlọ ọgwụ na-agwọ ọrịa, Ngalaba Na-ahụ Maka Ọgwụ, Ụlọ Ọgwụ Xiangya, Central South University) na Wang Ruoguang (Dọkịta nke Medicine, postdoctoral na biology, Changsha Ruoguang Medical Research Center) dekwara na: na usoro entecavir, e nwere ike were entecavir. ruo ọtụtụ afọ ma ọ bụ ọbụna afọ 10.Ihe karịrị afọ.Na enwere ike iji ya mee ihe site na ndị inyom dị ime, na-egosi nchekwa dị mma.

Na-ekpe ikpe site na usoro ọgwụ ọgwụ ndị a maara, Entecavir nwere ike inwe mmetụta antiviral sara mbara, ọ bụghị naanị dị irè megide HBV.

Anyị na-ejikarị Entecavir agwọ ọrịa na-efe efe nke iku ume n'ụlọọgwụ, mmetụta ya dị ịrịba ama.

Ka ọ dị ugbu a, na nyochaghachi ihe karịrị ndị ọrịa COVID19 500 na Hubei (ebe), naanị otu onye were entecavir.Oge ndenye ọgwụ bụ na mbido Jenụwarị, wee kwụsị ọgwụ ahụ.

Mgbe ị na-akwado ndị ọrụ ahụike na Hubei, ụfọdụ ndị dọkịta, ma ọ bụ ndị nwere ihe egwu dị elu, na-eji Entecavir ugbu a iji gbochie COVID19, enweghị ọrịa ọ bụla.Ndị mmadụ na-enyo enyo na-ewere entecavir, ọ nweghị onye nwere ọganihu ka a chọpụta ya na COVID19.

Okwu patent:

E nwere tumadi abụọ usoro, 06 usoro na 89 usoro.Mkpebi nke patent maka usoro 06 dị n'oge (na-agwụ na 2023)!Ọ bụ ezie na ọnụ ahịa nke usoro ahụ dị ntakịrị, àgwà ahụ dị mma, ndị ọrụ ahụ nwekwara ike ịdị ike, ndụmọdụ onwe onye: Maka osisi kemịkal, jiri usoro 06 mee ka ọ ghara ịdị mpako;maka ụlọ ọrụ ndị na-emepụta ọgwụ, ewepụla ihe ọ bụla ma ghara ịdị ize ndụ.

Na 2014, Chia Tai Tianqing nwetara ahịa kwa afọ nke ijeri yuan 10 site na ịdabere na ọgwụ nje dị ka entecavir, nke entecavir bụ 20%.

Ebe ọ bụ na a kwadoro entecavir maka mbubata na 2005, ihe karịrị ụlọ ọrụ ọgwụ ụlọ 100 etinyela akwụkwọ maka ndebanye aha ngwaahịa;N'ime ha, ụlọ ọrụ mmepụta ihe akwadoro gụnyere Jiangsu Zhengda Tianqing Pharmaceutical (nṅomi mbụ), Hainan Zhonghe Pharmaceutical, na Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical Siharmaceutical, Shanghai, Suzhou Dawnrays Pharmaceutical, Shanghai. ceutical, Shandong 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, wdg .;N'ihu site na ụbọchị nkwekọrịta, ngwaahịa a abanyela n'ọkwa nke ụdị ekwuputara ewu ewu kemgbe 2007.

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