Entecavir USP Impurity B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;

ʻO ka wehewehe pōkole:

Huahana Huahana

Palapala noi

Entecavir（SQ 34676;ʻO ka BMS 200475） ka mea hoʻokae HBV koho a maikaʻi.Ma nā pūnaewele HepG2 EC50 waiwai he 3.75 nM.ʻO nā lāʻau anti-hepatitis B hou loa a me ka anti-AIDS laina mua.

Entecavir hopena

ʻO kēia huahana he guanine nucleoside analog, nona ka hopena pale i ka maʻi hepatitis B (HBV) polymerase.Hiki ke phosphorylated i loko o ka triphosphate ikaika, a ʻo ka hapalua o ke ola o ka triphosphate i loko o ke kelepona he 15 mau hola.Ma ka hoʻokūkū ʻana me ka substrate kūlohelohe deoxyguanosine triphosphate o HBV polymerase, hiki i ka entecavir triphosphate ke kāohi i nā hana ʻekolu o ka polymerase viral (reverse transcriptase): (1) HBV polymerase initiation;(2) pregenomic mRNA Ka hoʻokumu ʻana o ke kaula maikaʻi ʻole o ka transcription hoʻohuli;(3) ʻO ka synthesis o ke kaula maikaʻi o HBV DNA.He 0.0012μM ka hoʻopaʻa mau (Ki) o entecavir triphosphate ma HBV DNA polymerase.ʻO Entecavir triphosphate ka hopena hoʻonāwaliwali i ka cell α, β, δ DNA polymerase a me ka mitochondrial γ DNA polymerase, me ka waiwai Ki o 18 a 160 μM.

Nā ʻāpana

E wehewehe	Entecavir（SQ 34676;ʻO BMS 200475）ʻo ia ka HBV Inhibitor koho a maikaʻi. Ma nā pūnaewele HepG2 EC50 ka waiwai he 3.75 nM.
Piliwaeʻano	ala hōʻailona >> Anti-infective >> HBV Research areas >> Infect
Kuhikuhi	EC50: 3.75 nM (anti-HBV, HepG2 cell)[2]
In vitronā haʻawina	ʻO ka EC50 o BMS-200475 i ka HBV he 3.75 nM.Hoʻokomo ʻia ia i loko o ka HBV protein primers, a laila ua kāohi ʻia ka pae hoʻomaka o ka reverse transcriptase.ʻOi aku ka haʻahaʻa o ka hana antiviral o BMS-200475 ma mua o nā maʻi RNA a me DNA [1].Ke hoʻohālikelike ʻia me nā analog deoxyguanosine ʻē aʻe (penciclovir, ganciclovir, lobucavir a me acyclovir) a i ʻole lamivudine, ʻoi aku ka phosphorylated o ka entecavir i kāna metabolite ikaika.ʻO ka hapalua o ke ola intracellular o Entecavir he 15 mau hola [2].
I loko o vivonoiʻi	Hana ʻia ʻo BMS-200475 ma ka waha i kēlā me kēia lā me kahi maʻi mai ka 0.02 a i ka 0.5 mg / kg ke kaumaha o ke kino no 1 a 3 mau mahina, hiki ke hoʻemi pono i ke kiʻekiʻe o ka viremia woodchuck hepatitis (WHV) viremia i nā woodchucks maʻi maʻi [3].
Keleponahoʻokolohua	Hoʻomākaukau ʻia ʻo BMS 200475 i loko o ka phosphate buffered saline (PBS) a hoʻoheheʻe ʻia me kahi ʻano kūpono i loaʻa ka 2% fetal bovine serum.HepG2. waena .Ua hana ʻia ka helu HBV ma ka lā 10th [1].
Nā kuhikuhi	[1].Innaimo SF, et al.ʻO ka ʻike ʻana o BMS-200475 ma ke ʻano he mea paʻa a koho i ka maʻi hepatitis B.Nā ʻĀpana Antimicrob Chemother.1997 Iulai;41(7):1444-9.[2].Rivkin A, et al.He loiloi o entecavir i ka mālama ʻana i ka maʻi hepatitis B mau.Curr Med Res Opin.2005 Nov;21(11):1845-57.[3].ʻO Genovesi EV, et al.Ka pono o ka carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 i loko o ke kumu hoʻohālike woodchuck o ka maʻi maʻi hepatitis B.Nā ʻĀpana Antimicrob Chemother.1998 Dek;42(12):3209-18.

Nā waiwai kino a me nā kemika o Entecavir

ʻO ka mānoanoa	1.8±0.1 g/cm³
Lae paila	734.2ºC ma 760 mmHg
Lae hehee	249-252ºC
ʻAno molekala	C12H15N5O3
Kaumaha molekula	277.279
Kuhikuhi uila	397.9ºC
ʻO ka maikaʻi pololei	277.117493
PSA	130.05000
LogP	-0.96
Nā hiʻohiʻona hiʻohiʻona	Keʻokeʻo a keʻokeʻo keʻokeʻo/melemele ka pauka kristal
Hōʻike hōʻike	1.837
Nā kūlana mālama	-20°C Pahu hau

Ka Dute Entecavir

Code dute	2933990099
Nānā Kūlana Pākē	2933990099. Nā pūhui heterocyclic ʻē aʻe i loaʻa nā heteroatoms nitrogen wale nō.Laki ʻauhau hoʻohui waiwai: 17.0%.Laki ʻauhau: 13.0%.Nā kūlana hoʻoponopono: ʻAʻohe.ʻO ka uku o ka lāhui i makemake nui ʻia: 6.5%.Ka uku nui: 20.0%
Nā mea hoʻolaha	ʻO ka inoa o ka huahana, ka mea hoʻohui, hoʻohana, hexamethylene chloride, e ʻoluʻolu e hōʻike i ke ʻano, 6-caprolactam, e ʻoluʻolu e hōʻike i ke ʻano, ka lā kau inoa.
Hōʻuluʻulu manaʻo	2933990090. nā pūhui heterocyclic me (s) nitrogen hetero-atom wale nō.VAT:17.0%.Laki ʻauhau: 13.0%..Ka uku MFN: 6.5%.Ka uku nui: 20.0%

ʻIke hou aku:

ʻO Qu Qiang (PhD i ka lāʻau lapaʻau lāʻau lapaʻau, Keʻena o Pharmacy, Xiangya Hospital, Central South University) a me Wang Ruoguang (Doctor of Medicine, postdoctoral in biology, Changsha Ruoguang Medical Research Center) i kākau pū ʻia: i ka entecavir regimen, hiki ke lawe ʻia ka entecavir no kekahi mau makahiki a i ʻole 10 mau makahiki.ʻOi aku ma mua o nā makahiki.A hiki ke hoʻohana ʻia e nā wahine hāpai, e hōʻike ana i ka palekana maikaʻi.

Ma ka hoʻoholo ʻana mai kēia mau hana lāʻau lapaʻau molecular i ʻike ʻia, hiki i ka Entecavir ke loaʻa i kahi hopena antiviral ākea ākea, ʻaʻole kūpono wale i ka HBV.

Hoʻohana pinepine mākou i ka Entecavir no ka mālama ʻana i nā maʻi hanu viral i loko o ke keʻena, a he mea kupaianaha ka hopena.

I kēia manawa, ma kahi loiloi retrospective o nā mea maʻi ma mua o 500 COVID19 ma Hubei (kahi), hoʻokahi wale nō kanaka i lawe i ka entecavir.ʻO ka manawa kuhikuhi i ka hoʻomaka o Ianuali, a laila ua hoʻopau ʻia ka lāʻau.

ʻOiai ke kākoʻo nei i nā limahana lapaʻau ma Hubei, kekahi mau kauka o ka ʻāina, a i ʻole nā hui kiʻekiʻe, ke hoʻohana nei i ka Entecavir e pale i ka COVID19, ʻaʻohe hihia o ka maʻi.ʻO ka poʻe i manaʻo ʻia e lawe i ka entecavir, ʻaʻohe mea i holomua e ʻike ʻia me COVID19.

Nā pilikia patent:

ʻElua mau kaʻina hana, 06 kaʻina a me 89 kaʻina.ʻO ka pau ʻana o ka patent no ke kaʻina hana 06 ʻoi loa (e pau i ka makahiki 2023)!ʻOiai he haʻahaʻa ke kumukūʻai o ke kaʻina hana, ʻoi aku ka maikaʻi o ka maikaʻi, a hiki i nā limahana ke ikaika, ʻōlelo aʻoaʻo pilikino: No nā mea kanu kemika, e hoʻohana i ka hana 06 ʻaʻole e haʻaheo;no nā hui lāʻau lapaʻau, ʻaʻole e lawe i ka puʻuwai a ʻaʻole hoʻi e hoʻoweliweli.

I ka makahiki 2014, ua hoʻokō ʻo Chia Tai Tianqing i nā kūʻai makahiki he 10 biliona yuan ma o ka hilinaʻi ʻana i nā lāʻau lapaʻau e like me entecavir, nona ka entecavir no 20%.

Ma muli o ka ʻae ʻia ʻana o ka entecavir no ka lawe ʻana mai i ka makahiki 2005, ʻoi aku ma mua o 100 mau hui lāʻau lapaʻau kūloko i noi no ke kākau inoa ʻana o ka huahana;i waena o lākou, nā hui hana i ʻae ʻia ʻo Jiangsu Zhengda Tianqing Pharmaceutical (hoʻohālikelike mua), Hainan Zhonghe Pharmaceutical, a 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.;mai ka lā o ka ʻaelike, ua komo kēia huahana i nā kūlana o nā ʻano kaulana kaulana mai 2007.

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Mua: p-Tolylcarboxylic acid;4-Toluic acid,99%;4-Carboxytoluene, p-Toluic acid;

Aʻe: FondaparinSodiuM;Fondaparinux SodiuM Identification;Fondaparinux sodium N-4;

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