Entecavir USP Le mama B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

Fa'amatalaga Puupuu:

Fa'amatalaga Oloa

Faailoga o oloa

Fa'aaogāga

Entecavir（SQ 34676;BMS 200475）o le HBV Inhibitor filifilia ma aoga.I sela HepG2 EC50 tau o le 3.75 nM.O vaila'au fa'ato'a fa'ato'a fou e fa'ama'i-hepatitis B ma fa'ama'i-AIDS.

Entecavir aafiaga

O lenei oloa o le guanine nucleoside analog, lea e iai sona aafiaga fa'alavelave ile siama ole hepatitis B (HBV) polymerase.E mafai ona phosphorylated i triphosphate malosi, ma o le afa-ola o le triphosphate i le sela e 15 itula.E ala i le tauva ma le HBV polymerase's natural substrate deoxyguanosine triphosphate, e mafai e le entecavir triphosphate ona taofia gaoioiga uma e tolu a viral polymerase (reverse transcriptase): (1) HBV polymerase initiation;(2) pregenomic mRNA Le fa'avaeina o le fa'asologa o le fa'asologa fa'asolosolo;(3) Le tu'ufa'atasiga o le manoa lelei o le HBV DNA.O le fa'alavelave fa'alavelave (Ki) ole entecavir triphosphate ile HBV DNA polymerase ole 0.0012μM.Entecavir triphosphate e vaivai le a'afiaga i le cell α, β, δ DNA polymerase ma le mitochondrial γ DNA polymerase, ma le Ki tau o le 18 i le 160 μM.

Parameter

Faamatala	Entecavir（SQ 34676;BMS 200475）o le HBV Inhibitor filifilia ma aoga. I sela HepG2 EC50 tau o le 3.75 nM.
Fa'atatauvaega	ala faailo >> Anti-fa'ama'i >> HBV Su'esu'ega nofoaga >> A'afia
Sini	EC50: 3.75 nM (anti-HBV, sela HepG2)[2]
In vitrosu'esu'ega	Ole EC50 ole BMS-200475 ile HBV ole 3.75nM.O lo'o tu'ufa'atasia i totonu ole HBV protein primers, ona taofia lea ole la'asaga amata ole reverse transcriptase.Ole gaioiga antiviral ole BMS-200475 e matua maualalo lava nai lo isi siama RNA ma DNA [1].Pe a faatusatusa i isi analogs deoxyguanosine (penciclovir, ganciclovir, lobucavir ma acyclovir) poʻo le lamivudine, entecavir e sili atu ona phosphorylated i lona metabolite malosi.Ole afa ole ola ole intracellular ole Entecavir e 15 itula [2].
I vivosu'esu'ega	BMS-200475 e togafitia tautala i aso uma ma se fua e amata mai i le 0.02 i le 0.5 mg / kg mamafa o le tino mo le 1 i le 3 masina, lea e mafai ona faʻaitiitia lelei ai le maualuga o le viremia o le woodchuck hepatitis virus (WHV) i faʻamaʻi pipisi masani [3].
selafa'ata'ita'iga	BMS 200475 o lo'o saunia ile phosphate buffered saline (PBS) ma fa'afefete i se ala talafeagai e iai le 2% fetal bovine serum.HepG2 2.2.15 sela na fatu i luga o le 12-well Biocoat collagen-coated plate i le mamafa o le 5 × 10 5 sela i le vaieli, ma teuina i se tulaga faʻafefiloi mo le 2 i le 3 aso, ona ufiufi lea i le 1 mL o le BMS 200475. feololo .O le fa'atusatusaina o le HBV na faia i le aso 10 [1].
Fa'asinomaga	[1].Innaimo SF, et al.Fa'ailoaina o le BMS-200475 o se fa'atosina malosi ma filifili ole siama ole hepatitis B.Antimicrob Agents Chemother.1997 Iul;41(7):1444-9.[2].Rivkin A, et al.O se toe iloiloga o le entecavir i le togafitiga o faʻamaʻi pipisi o le hepatitis B.Curr Med Res Opin.2005 Nov;21(11):1845-57.[3].Genovesi EV, et al.Le aoga o le carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 i le woodchuck faʻataʻitaʻiga o le hepatitis B siama siama.Antimicrob Agents Chemother.1998 Tesema;42(12):3209-18.

Fa'aletino ma kemisi o le Entecavir

Malosi	1.8±0.1 g/cm³
Fa'apuna	734.2ºC ile 760 mmHg
Liu liusuavai	249-252ºC
fua mole	C12H15N5O3
mamafa mole	277.279
Fa'ailoga moli	397.9ºC
Tulaga sa'o	277.117493
PSA	130.05000
LogP	-0.96
Uiga foliga	Pa'epa'e ile pa'epa'e/samasama pa'u tioata
Fa'ailoga fa'afofo	1.837
Tulaga teuina	-20°C pusaaisa

Entecavir Customs

Tulafono a le Ofisa o Tiute	2933990099
Vaaiga Fa'aSaina	2933990099. O isi fa'apotopotoga fa'ata'ita'i o lo'o i ai na'o le nitrogen heteroatoms.Lafoga fa'aopoopo o tau: 17.0%.Lafoga toe fa'aitiitiga: 13.0%.Tulaga fa'atonutonu: Leai.Totogi sili ona fiafia i ai le atunuu: 6.5%.Totogi lautele: 20.0%
Elemene ta'utinoga	Igoa o oloa, mea e aofia ai, faʻaoga, hexamethylene chloride, faʻamolemole faʻaalia foliga vaaia, 6-caprolactam, faʻamolemole faʻaalia foliga vaaia, aso saini
Aotelega	2933990090. fa'atasiga fa'agata fa'atasi ma na'o le fa'aato-atoma.VAT:17.0%.Lafoga fa'aitiitiga fua faatatau:13.0%..MFN tau:6.5%.Totogi lautele:20.0%

Fa'amatalaga fa'aopoopo:

Qu Qiang (PhD i falemaʻi falemaʻi, Matagaluega o Falemaʻi, Falemai Xiangya, Iunivesite i Saute Tutotonu) ma Wang Ruoguang (Fomaʻi Fomai, postdoctoral i le biology, Changsha Ruoguang Medical Research Center) na tusia foi e faapea: i le entecavir regimen, entecavir e mafai ona ave. mo ni nai tausaga po o le 10 tausaga.E sili atu nai lo tausaga.Ma e mafai ona faʻaaogaina e fafine maʻitaga, faʻaalia le saogalemu lelei.

Ile fa'amasinoina mai nei molecular pharmacological mechanisms, Entecavir e mafai ona i ai se fa'alavelave fa'ama'i lautele, e le gata ina aoga i le HBV.

E masani foi ona matou faʻaogaina le Entecavir e togafitia ai faʻamaʻi pipisi o le manava i totonu o le falemaʻi, ma e ofoofogia le aafiaga.

I le taimi nei, i se iloiloga lata mai o le silia ma le 500 COVID19 gasegase i Hubei (se nofoaga), naʻo le tasi le tagata na ave le entecavir.O le taimi o talavai o le amataga o Ianuari, ona taofi lea o le fualaau.

A o lagolagoina le aufaigaluega fomaʻi i Hubei, o nisi o fomaʻi, poʻo vaega e maualuga le lamatiaga, o loʻo faʻaogaina nei le Entecavir e puipuia ai le COVID19, e leai se faʻamaʻi pipisi.O tagata masalomia o loʻo ave le entecavir, e leai se tasi ua alualu i luma e maua i le COVID19.

mataupu pateni:

E masani ona lua faiga, 06 faagasologa ma 89 faagasologa.O le mutaaga o le pateni mo le 06 faagasologa ua vave tele (e muta i le 2023)!E ui lava o le tau o le faagasologa e maualalo, o le tulaga lelei e fai si lelei, ma e mafai e le aufaigaluega ona malosi, fautuaga a le tagata lava ia: Mo vailaʻau vailaʻau, faʻaoga le 06 faiga e aua le faʻamaualuga;mo kamupani vaila'au, 'aua ne'i fa'atauva'a ma 'aua ne'i fa'amata'u tele .

I le 2014, na ausia ai e Chia Tai Tianqing le faʻatauga faʻaletausaga o le 10 piliona yuan e ala i le faʻalagolago i vailaʻau faʻapitoa e pei o le entecavir, lea e entecavir e 20%.

Talu ai na faʻamaonia le entecavir mo le faʻaulufaleina mai i le 2005, e sili atu i le 100 kamupani faʻatau oloa i totonu o le atunuʻu ua talosaga mo le resitalaina o le oloa;faatasi ai ma i latou, o le kamupani gaosiga faamaonia e aofia ai Jiangsu Zhengda Tianqing Pharmaceutical (muamua faafoliga), Hainan Zhonghe Pharmaceutical, ma Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Qingsong Pharmaceutical, Sichuan Haiscoutical 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, ma isi;mai le aso o le konekarate, o lenei oloa ua ulufale atu i tulaga o lauiloa lauiloa ituaiga talu mai le 2007.

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