Entecavir USP Impurity B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir USP Impurity B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir (SQ 34676;BMS 200475) yog xaiv thiab siv tau HBV Inhibitor.Hauv HepG2 hlwb EC50 tus nqi yog 3.75 nM.Cov tshuaj tiv thaiv kab mob siab B thiab tshuaj tiv thaiv kab mob AIDS thawj zaug.
Cov nyhuv Entecavir
Cov khoom no yog guanine nucleoside analog, uas muaj cov nyhuv inhibitory ntawm tus kab mob siab B (HBV) polymerase.Nws tuaj yeem raug phosphorylated rau hauv lub cev muaj zog triphosphate, thiab ib nrab-lub neej ntawm triphosphate hauv cell yog 15 teev.Los ntawm kev sib tw nrog HBV polymerase lub ntuj substrate deoxyguanosine triphosphate, entecavir triphosphate tuaj yeem cuam tshuam tag nrho peb cov dej num ntawm viral polymerase (reverse transcriptase): (1) HBV polymerase pib;(2) pregenomic mRNA Qhov tsim ntawm qhov tsis zoo strand ntawm thim rov qab;(3) Lub synthesis ntawm qhov zoo strand ntawm HBV DNA.Qhov inhibitory tas li (Ki) ntawm entecavir triphosphate ntawm HBV DNA polymerase yog 0.0012μM.Entecavir triphosphate muaj zog inhibitory nyhuv ntawm cell α, β, δ DNA polymerase thiab mitochondrial γ DNA polymerase, nrog Ki nqi ntawm 18 mus rau 160 μM.
| Piav | Entecavir (SQ 34676;BMS 200475) yog xaiv thiab siv tau HBV Inhibitor.In HepG2 hlwb EC50 tus nqi yog 3.75 nM. |
| Hais txogpawg | teeb liab txoj kev >> Tshuaj tiv thaiv kab mob >> HBV Kev tshawb fawb thaj chaw >> Kab mob |
| Hom phiaj | EC50: 3.75 nM (anti-HBV, HepG2 cell)[2] |
| Hauv vitrokev kawm | EC50 ntawm BMS-200475 rau HBV yog 3.75 nM.Nws tau muab tso rau hauv HBV protein primers, thiab tom qab ntawd cov kauj ruam pib ntawm thim rov qab transcriptase yog inhibited.Cov tshuaj tiv thaiv kab mob ntawm BMS-200475 yog qhov qis dua li lwm cov kab mob RNA thiab DNA [1].Piv nrog rau lwm yam deoxyguanosine analogues (penciclovir, ganciclovir, lobucavir thiab acyclovir) los yog lamivudine, entecavir feem ntau yuav phosphorylated rau nws cov nquag metabolite.Intracellular ib nrab-lub neej ntawm Entecavir yog 15 teev [2]. |
| Hauv vivokev tshawb fawb | BMS-200475 tau kho qhov ncauj txhua hnub nrog koob tshuaj ntawm 0.02 txog 0.5 mg / kg lub cev qhov hnyav rau 1 mus rau 3 lub hlis, uas tuaj yeem txo qis tus kab mob woodchuck hepatitis virus (WHV) viremia hauv cov ntoo chucks ntev [3]. |
| Cellkev sim | BMS 200475 yog npaj nyob rau hauv phosphate buffered saline (PBS) thiab diluted nrog ib tug tsim nyog nruab nrab uas muaj 2% fetal bovine serum.HepG2 2.2.15 hlwb tau cog rau ntawm 12-zoo Biocoat collagen-coated phaj ntawm qhov ntom ntawm 5 × 10 5 hlwb rau ib qhov dej, thiab khaws cia rau hauv lub xeev sib xyaw rau 2 mus rau 3 hnub, thiab tom qab ntawd npog nrog 1 mL ntawm BMS 200475 nruab nrab.Kev ntsuas HBV tau ua rau hnub 10 [1]. |
| Cov ntaub ntawv | [1].Innaimo SF, et al.Kev txheeb xyuas ntawm BMS-200475 yog ib qho muaj zog thiab xaiv inhibitor ntawm tus kab mob siab B.Antimicrob Agents Chemother.1997 Lub Xya Hli; 41(7): 1444-9.Rivkin A, et al.Kev tshuaj xyuas ntawm entecavir hauv kev kho tus kab mob siab B mob ntev.Curr Med Res Opin.2005 Nov; 21(11): 1845-57[3].Genovesi EV, et al.Kev ua tau zoo ntawm carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 hauv woodchuck qauv ntawm kab mob siab B.Antimicrob Agents Chemother.1998 Dec; 42(12): 3209-18. |
Lub cev thiab tshuaj muaj zog ntawm Entecavir
| Qhov ntom | 1.8 ± 0.1g / cm33 |
| Boiling point | 734.2ºC ntawm 760 mmHg |
| Melting point | 249-252 ºC |
| Cov mis mos molecular | C12H15N5O3 |
| Molecular hnyav | 277.279 ib |
| Flash point | 397.9°C ib |
| Precise zoo | 277.117493 ib |
| PSA | 130.05.00 Nws |
| LogP | -0.96 |
| Cov tsos mob tshwm sim | Dawb rau tawm-dawb / daj crystalline hmoov |
| Refractive Index | 1.837 ib |
| Cia tej yam kev mob | -20 ° C Lub Freezer |
Entecavir Kev lis kev cai
| Kev lis kev cai code | 293390099 ib |
| Suav Txheej txheem cej luam | 2933990099. Lwm cov tshuaj heterocyclic uas muaj nitrogen heteroatoms xwb.Tus nqi se ntxiv: 17.0%.Tus nqi se rov qab: 13.0%.Regulatory tej yam kev mob: Tsis muaj.Feem ntau cov neeg nyiam tariff: 6.5%.Tus nqi se: 20.0% |
| Cov ntsiab lus tshaj tawm | Cov khoom npe, cov ntsiab lus muaj, siv, hexamethylene chloride, thov qhia qhov tsos, 6-caprolactam, thov qhia qhov tsos, kos npe hnub |
| Cov ntsiab lus | 2933990090. heterocyclic compounds nrog nitrogen hetero-atom(s) nkaus xwb.VAT: 17.0%.Tus nqi se rov qab: 13.0%..MFN tariff: 6.5%.Tus nqi se: 20.0% |
Cov ntaub ntawv ntxiv:
Qu Qiang (PhD nyob rau hauv chaw kho mob pharmacology, Department of Pharmacy, Xiangya Tsev Kho Mob, Central South University) thiab Wang Ruoguang (tus kws kho mob ntawm cov tshuaj, postdoctoral nyob rau hauv biology, Changsha Ruoguang Medical Research Center) kuj sau hais tias: nyob rau hauv lub entecavir regimen, entecavir tuaj yeem noj. rau ntau xyoo lossis txawm tias 10 xyoo.Ntau tshaj xyoo.Thiab nws tuaj yeem siv los ntawm cov poj niam cev xeeb tub, qhia txog kev nyab xeeb zoo.
Kev txiav txim los ntawm cov kev paub txog cov tshuaj molecular pharmacological, Entecavir tuaj yeem muaj cov tshuaj tiv thaiv kab mob dav dav, tsis yog tsuas yog tiv thaiv HBV xwb.
Peb kuj feem ntau siv Entecavir los kho cov kab mob ua pa hauv cov chaw kho mob, thiab cov txiaj ntsig zoo kawg li.
Tam sim no, hauv kev tshuaj xyuas rov qab ntawm ntau dua 500 tus neeg mob COVID19 hauv Hubei (ib qho chaw), tsuas yog ib tus neeg tau noj entecavir.Lub sijhawm tshuaj yog nyob rau lub Ib Hlis thaum ntxov, thiab tom qab ntawd cov tshuaj tau tso tseg.
Thaum txhawb nqa cov neeg ua haujlwm kho mob hauv Hubei, qee tus kws kho mob hauv paus, lossis pab pawg muaj kev pheej hmoo siab, tam sim no siv Entecavir los tiv thaiv COVID19, tsis muaj tus kabmob kis.Cov neeg raug liam tias noj entecavir, tsis muaj leej twg tau nce mus kuaj pom tus mob COVID19.
Patent teeb meem:
Muaj ob txheej txheem, 06 txheej txheem thiab 89 txheej txheem.Lub sijhawm tas sijhawm ntawm patent rau 06 txheej txheem yog ntxov dhau (tshaj tawm xyoo 2023)!Txawm hais tias tus nqi ntawm cov txheej txheem yog tsawg, qhov zoo yog qhov zoo, thiab cov neeg ua haujlwm tuaj yeem muaj zog, cov lus qhia ntawm tus kheej: Rau cov nroj tsuag tshuaj, siv cov txheej txheem 06 kom tsis txhob khav theeb heev;rau cov tuam txhab tshuaj, tsis txhob noj cov tshuaj fluke thiab tsis txhob muaj kev pheej hmoo.
Hauv xyoo 2014, Chia Tai Tianqing tau ua tiav kev muag khoom txhua xyoo ntawm 10 billion yuan los ntawm kev tso siab rau cov tshuaj nquag xws li entecavir, ntawm qhov uas entecavir suav txog 20%.
Txij li thaum entecavir tau pom zoo rau kev ntshuam hauv xyoo 2005, ntau tshaj 100 lub tuam txhab tshuaj hauv tsev tau thov rau kev tso npe ntawm cov khoom;ntawm lawv, cov tuam txhab tsim khoom tau pom zoo suav nrog Jiangsu Zhengda Tianqing Pharmaceutical (thawj hais lus), Hainan Zhonghe Pharmaceutical, thiab Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Qingscormicutical 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, thiab lwm yam.;ntxiv los ntawm hnub ntawm daim ntawv cog lus, cov khoom no tau nkag mus rau hauv qeb ntawm nrov tshaj tawm ntau yam txij li thaum 2007.
JIN DUN Medical muajISO tsim nyog thiab ua tau raws li GMP cov qauv tsim, ua hauj lwm hauv tsev thiab txawv teb chaws cov kws kho tshuaj synthesis nrog kev nplua nuj los coj lub tuam txhab R & D.
TECHNOL OGY ADVANTAGES
● High Pressure Catalytic Hydrogenation .High Pressure Hydrogenolysis Reaction.Cryogenic cov tshuaj tiv thaiv (<-78% C)
●Aromatic Heterocyclic Synthesis
● Kev Ruaj Ntseg Tsis Zoo
● Chiral Resolution
●Heck, Suzuki, Negishi, Sonogashira .Gignard Reaction
Cov khoom siv
Peb lub Lab muaj ntau yam kev sim thiab ntsuas cov cuab yeej, xws li: NMR (Bruker 400M), HPLC, chiral-HPLC, LC-MS, LC-MS/MS (API 4000), IR, UV, GC, GC-MS, Chromatography, Microwave Synthesizer, Parallel Synthesizer, Differential Scanning Calorimeter (DSC), Electron Microscope ...
Pab neeg R&D
Jindun Kev Kho Mob muaj ib pab pawg kws tshaj lij R & D cov neeg ua haujlwm, thiab ntiav ntau tus kws tshaj lij kev siv tshuaj hauv tsev thiab txawv teb chaws los coj R&D, ua rau peb cov khoom sib xyaw ua kom raug thiab ua tau zoo.
Peb tau pab ntau lub tuam txhab tshuaj hauv tsev sab saum toj, xws liHansoh, Hengrui thiab HEC Pharm.Ntawm no peb yuav qhia ib feem ntawm lawv.
Customzation Case Ib:
CAS Nr .: 110351-94-5
Customzation Case Ob:
CAS Nr .: 144848-24-8
Customzation Case Peb:
CAS Nr .: 200636-54-0
1.Customize New Intermediates lossis APIs.Ib yam li cov ntaub ntawv sib qhia saum toj no, cov neeg siv khoom muaj qhov xav tau tshwj xeeb Intermediates lossis APIs, thiab lawv nrhiav tsis tau cov khoom xav tau hauv khw, ces peb tuaj yeem pab kho.
2.Txheej txheem Optimization rau cov khoom qub.Peb pab neeg yuav pab Optimize thiab txhim kho xws li ntau lawm uas nws cov tshuaj tiv thaiv txoj kev yog qub, ntau lawm nqi yog siab, thiab efficiency yog tsawg.Peb tuaj yeem muab cov ntaub ntawv tag nrho rau kev hloov pauv thev naus laus zis thiab kev txhim kho cov txheej txheem, pab cov neeg siv khoom kom muaj txiaj ntsig ntau dua.
Los ntawm cov hom phiaj tshuaj rau INDs, JIN DUN Kev Kho Mob muab rau kojib-nres tus kheej R & D kev daws teeb meem.
JIN DUN Kev Kho Mob hais kom tsim ib pab neeg nrog kev npau suav, ua cov khoom muaj txiaj ntsig, ua kom zoo, nruj, thiab tawm mus ua ib tus neeg ntseeg siab thiab phooj ywg ntawm cov neeg siv khoom!
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