Entecavir USP wasakh B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir USP wasakh B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir (SQ 34676;BMS 200475) waa xushay oo waxtar leh HBV Inhibitor.Unugyada HepG2 qiimaha EC50 waa 3.75 nM.Dawooyinkii ugu dambeeyay ee ka hortagga cagaarshowga B iyo ka-hortagga AIDS-ka.
saamaynta Entecavir
Alaabtani waa analooga guanine nucleoside, kaas oo saameyn joojin ku leh fayraska cagaarshow B (HBV) polymerase.Waxaa lagu shubi karaa fosfooraska firfircoon ee triphosphate, iyo nuska nolosha triphosphate ee unugga waa 15 saacadood.Iyada oo la tartamaysa HBV polymerase substrate-ka dabiiciga ah ee deoxyguanosine triphosphate, entecavir triphosphate waxay joojin kartaa dhammaan saddexda hawlood ee polymerase fayraska (transcriptase roga): (1) HBV polymerase bilaabista;(2) pregenomic mRNA Samaynta xuddunta taban ee qoraalka gadaasha;(3) Isku-dubaridka xadhigga togan ee HBV DNA.Joogtada xannibaadda (Ki) ee triphosphate entecavir ee HBV DNA polymerase waa 0.0012μM.Entecavir triphosphate waxay leedahay saameyn daciif ah oo ka hortag ah unugyada α, β, δ DNA polymerase iyo mitochondrial γ DNA polymerase, oo leh qiimaha Ki ee 18 ilaa 160 μM.
| Sharax | Entecavir (SQ 34676;BMS 200475) waa mid door ah oo waxtar leh HBV Inhibitor. Unugyada HepG2 ee EC50 qiimaha waa 3.75 nM. |
| la xidhiidhaqaybaha | Jidka calaamadda >> Ka-hortagga caabuqa >> HBV meelaha cilmi-baarista >> Fayraska |
| Bartilmaameedka | EC50: 3.75 nM (ka-hortagga HBV, unugga HepG2)[2] |
| In vitrowaxbarashada | EC50 ee BMS-200475 ilaa HBV waa 3.75 nM.Waxa lagu daraa aasaasayaasha borotiinka HBV, ka dibna tallaabada bilawga ah ee qoraalka qoraalka ah waa la xannibay.Dhaqdhaqaaqa ka hortagga fayraska ee BMS-200475 aad ayuu uga hooseeyaa fayraska kale ee RNA iyo DNA [1].Marka la barbardhigo analogs kale ee deoxyguanosine (penciclovir, ganciclovir, lobucavir iyo acyclovir) ama lamivudine, entecavir waxay u badan tahay in lagu daro fosforyaalka metabolite firfircoon.Nolosha nuska unugyada gudaha ee Entecavir waa 15 saacadood [2]. |
| In vivocilmi baaris | BMS-200475 waxaa lagu daaweeyaa afka maalin kasta iyada oo qiyaasta u dhaxaysa 0.02 ilaa 0.5 mg / kg miisaanka jidhka 1 ilaa 3 bilood, taas oo si wax ku ool ah u yareyn karta heerka fayraska cagaarshowga woodchuck (WHV) ee fayrasyada ku jira woodchucks joogto ah [3]. |
| Unugtijaabo | BMS 200475 waxaa lagu diyaariyaa cusbada fosfooraska buffered (PBS) waxaana lagu qasi jiray dhexdhexaad ku habboon oo ka kooban 2% serum lo'da uurjiifka.Unugyada HepG2 2.2.15 waxaa lagu beeray saxan 12-wanaagsan Biocoat collagen-dahaarka leh cufnaanta 5 × 10 5 unug kasta, waxaana lagu hayaa xaalad isku dhafan 2 ilaa 3 maalmood, ka dibna lagu daboolay 1 mL ee BMS 200475 dhexdhexaad ah .Qiyaasta HBV waxa la sameeyay maalintii 10aad [1]. |
| Tixraacyo | [1]Inamo SF, iyo al.Aqoonsiga BMS-200475 inuu yahay horjooge awood leh oo doorta fayraska cagaarshow B.Kiimikada wakiilada Ka-hortagga ah.1997 Jul;41(7):1444-9.[2].Rivkin A, iyo al.Dib u eegis ku saabsan entecavir ee daawaynta infekshanka cagaarshow B raaga.Curr Med Res Opin.2005 Nof;21 (11): 1845-57.[3].Genovesi EV, iyo al.Waxtarka karbocyclic 2'-deoxyguanosine nucleoside BMS-200475 ee qaabka woodchuck ee caabuqa fayraska cagaarshow B.Kiimikada wakiilada Ka-hortagga ah.1998 Dec;42 (12):3209-18. |
Astaamaha jireed iyo kiimikaad ee Entecavir
| Cufnaanta | 1.8±0.1 g/cm3 |
| Barta karkarinta | 734.2ºC at 760 mmHg |
| barta dhalaalaysa | 249-252ºC |
| qaacidada molecular | C12H15N5O3 |
| Miisaanka molecular | 277.279 |
| Barta toosan | 397.9ºC |
| Tayada saxda ah | 277.117493 |
| PSA | 130.05000 |
| LogP | -0.96 |
| Astaamaha muuqaalka | Caddaan ama budo crystalline ah oo jaale ah |
| Tilmaanta refractive | 1.837 |
| Xaaladaha kaydinta | -20°C qaboojiyaha |
Kastamka Entecavir
| Koodhka kastamka | 2933990099 |
| Dulmarka Shiinaha | 2933990099. Xeryaha kale ee heterocyclic oo ay ku jiraan heteroatoms nitrogen oo kaliya.Qiimaha canshuurta lagu daray: 17.0%.Heerka dhimista canshuurta: 13.0%.Shuruudaha sharciyeed: Midna.Tacriifada qaranka ee ugu caansan: 6.5%.Qiimaha guud: 20.0% |
| Qodobbada caddaynta | Magaca badeecada, waxyaabaha ka kooban, isticmaalka, hexamethylene chloride, fadlan muuji muuqaalka, 6-caprolactam, fadlan muuji muuqaalka, taariikhda saxeexa |
| Soo koobid | 2933990090. Xeryahooda heterocyclic oo leh nitrogen hetero-atom(yada) kaliya.VAT: 17.0%.Heerka dhimista canshuurta: 13.0%..Qiimaha MFN:6.5%.Qiimaha guud: 20.0% |
Xog dheeraad ah:
Qu Qiang (PhD ee farmashiyaha kiliinikada, Waaxda Farmashiyaha, Isbitaalka Xiangya, Jaamacadda Bartamaha Koonfurta) iyo Wang Ruoguang (Dhakhtarka Daawada, Cilmi-baarista Caafimaadka ee Changsha Ruoguang) ayaa sidoo kale qoray: in nidaamka entecavir, entecavir la qaadan karo dhowr sano ama xitaa 10 sano.In ka badan sanado.Oo waxaa isticmaali kara haweenka uurka leh, oo muujinaya badbaado wanaagsan.
Marka la eego hababka farmasiga ee loo yaqaan molecular, Entecavir waxaa laga yaabaa inay leedahay saameyn ballaaran oo fayruska ka hortagga ah, oo aan waxtar u lahayn oo keliya HBV.
Waxaan sidoo kale inta badan u isticmaalnaa Entecavir si loogu daweeyo caabuqyada neef-mareenka fayraska ee rugta caafimaadka, saameyntuna waa mid cajiib ah.
Waqtigan xaadirka ah, dib-u-eegis dib-u-eegis lagu sameeyay in ka badan 500 oo bukaan COVID19 ah oo ku sugan Hubei (meel), hal qof oo keliya ayaa qaatay entecavir.Wakhtiga dhakhtarku qoray wuxuu ahaa horraantii Janaayo, ka dibna daawada waa la joojiyay.
Iyadoo la taageerayo shaqaalaha caafimaadka ee Hubei, qaar ka mid ah dhakhaatiirta asaasiga ah, ama kooxaha khatarta sare leh, oo hadda isticmaalaya Entecavir si looga hortago COVID19, ma jiro kiis caabuq ah.Dadka looga shakisan yahay inay qaadanayaan entecavir, qofna horumar uma samayn in laga helo COVID19.
Arrimaha shatiga:
Inta badan waxaa jira laba hab, 06 hab iyo 89 hab.Dhammaadka shatiyada ee habka 06 aad bay u dhakhso badan tahay (wuxuu dhacayaa 2023)!Inkasta oo qiimaha geeddi-socodku uu yar yahay, tayada ayaa ah mid aad u wanaagsan, shaqaaluhuna waxay noqon karaan kuwo xooggan, talo-bixin shakhsiyeed: Dhirta kiimikada, isticmaal habka 06 si aanad u kibrin;shirkadaha dawooyinka, ha ku daalin oo ha noqon mid aad khatar u ah.
Sannadkii 2014, Chia Tai Tianqing waxay gaadhay iib sannadkii 10 bilyan yuan iyada oo ku tiirsan dawooyinka guud sida entecavir, oo entecavir ay ka dhigan tahay 20%.
Tan iyo markii entecavir loo ogolaaday soo dejinta 2005, in ka badan 100 shirkadood oo dawooyinka gudaha ah ayaa codsaday diiwaangelinta alaabta;iyaga ka mid ah, shirkadaha wax soo saarka ee la ansixiyay waxaa ka mid ah Jiangsu Zhengda Tianqing Pharmaceutical (ku dayashada kowaad), Hainan Zhonghe Pharmaceutical, iyo Fujian Guangxi Pharmaceutical Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical Pharmaceutical, Suzhou Dawnrays Pharmaceutical Pharmaceutical Shanghai Ceutical, Shandong Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Biochemical.
Daawooyinka, Anhui Baker Biopharmaceutical, Hunan Concord Pharmaceutical Industry, Beijing Xiehe Pharmaceutical Factory, Beijing Baiao Pharmaceutical, Xinlitai Pharmaceutical, Dongyangguang, iwm .;Laga soo bilaabo taariikhda qandaraaska, badeecadani waxay gashay darajooyinka noocyada caanka ah ee lagu dhawaaqay tan iyo 2007.
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