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) inosarudza uye inoshanda HBV Inhibitor.MuHepG2 maseru EC50 kukosha ndeye 3.75 nM.Mishonga yemazuva ano inorwisa hepatitis B uye anti-AIDS yekutanga.
Entecavir mhedzisiro
Ichi chigadzirwa chinonzi guanine nucleoside analog, ine inhibitory effect pahutachiona hwehepatitis B (HBV) polymerase.Inogona kuva phosphorylated kuita triphosphate inoshanda, uye hafu yehupenyu hwe triphosphate muchitokisi maawa gumi nemashanu.Nokukwikwidzana neHBV polymerase's natural substrate deoxyguanosine triphosphate, entecavir triphosphate inogona kudzivisa mabasa ose matatu ehutachiona hwepolymerase (reverse transcriptase): (1) HBV polymerase initiation;(2) pregenomic mRNA Kuumbwa kweiyo yakaipa strand ye reverse transcription;(3) Kuumbwa kwetambo yakanaka yeHBV DNA.Iyo inhibitory constant (Ki) ye entecavir triphosphate paHBV DNA polymerase ndeye 0.0012μM.Entecavir triphosphate ine simba inhibitory effect pane cell α, β, δ DNA polymerase uye mitochondrial γ DNA polymerase, ine Ki kukosha kwe18 kusvika ku160 μM.
| Rondedzera | Entecavir (SQ 34676;BMS 200475) inosarudza uye inoshanda HBV Inhibitor.MuHepG2 maseru EC50 kukosha ndeye 3.75 nM. |
| Relatedmapoka | nzira yechiratidzo >> Anti-infective >> HBV Research nzvimbo >> Infect |
| Target | EC50: 3.75 nM (anti-HBV, HepG2 sero)[2] |
| In vitrozvidzidzo | Iyo EC50 yeBMS-200475 kusvika kuHBV ndeye 3.75 nM.Inosanganiswa muHBV protein primers, uye ipapo danho rekutanga reverse transcriptase rinodzivirirwa.Iyo antiviral chiitiko cheBMS-200475 yakaderera zvakanyanya kupfuura mamwe maRNA neDNA mavhairasi [1].Kuenzaniswa nedzimwe deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir uye acyclovir) kana lamivudine, entecavir inowanzoita phosphorylated kune metabolite yayo inoshanda.Iyo intracellular hafu yeupenyu yeEntecavir ndeye 15 maawa [2]. |
| In vivoresearch | BMS-200475 inobatwa nemuromo zuva rega rega nedoro kubva ku0.02 kusvika ku0.5 mg / kg uremu hwemuviri kwemwedzi 1 kusvika ku3, iyo inogona kunyatsodzikisa huwandu hwehunichuck hepatitis virus (WHV) viremia muhuni husina hutachiwana husingagumi [3]. |
| Seroexperiment | BMS 200475 inogadzirwa muphosphate buffered saline (PBS) uye yakanyungudutswa nepakati yakakodzera ine 2% fetal bovine serum.HepG2 2.2.15 masero akadyarwa pa 12-tsime Biocoat collagen-coated plate pa density ye 5 × 10 5 masero 5 patsime, uye akachengetwa munzvimbo yakasangana kwemazuva 2 kusvika 3, uyezve yakavharwa ne1 mL yeBMS 200475. pakati .HBV quantification yakaitwa pazuva regumi [1]. |
| References | [1].Innaimo SF, nevamwe.Kuzivikanwa kweBMS-200475 seine simba uye inosarudza inhibitor yehutachiona hweH hepatitis B.Antimicrob Agents Chemother.1997 Jul;41(7):1444-9[2].Rivkin A, nevamwe.Kuongororwa kwe entecavir mukurapa kwechirwere chisingaperi chehepatitis B.Curr Med Res Opin.2005 Nov;21(11):1845-57.[3].Genovesi EV, et al.Kubudirira kweiyo carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 muwoodchuck modhi yehutachiona hwehepatitis B.Antimicrob Agents Chemother.1998 Dec;42(12):3209-18. |
Zvenyama uye zvemakemikari zvimiro zveEntecavir
| Density | 1.8±0.1 g/cm3 |
| Boiling point | 734.2ºC pa760 mmHg |
| Melting point | 249-252ºC |
| Molecular formula | C12H15N5O3 |
| Molecular uremu | 277.279 |
| Flash point | 397.9ºC |
| Hunhu chaihwo | 277.117493 |
| PSA | 130.05000 |
| LogP | -0.96 |
| Chitarisiko hunhu | Ichena kusvika kune-chena / yero crystalline poda |
| Refractive index | 1.837 |
| Kuchengetedza mamiriro | -20°C Mufiriza |
Entecavir Customs
| Customs code | 2933990099 |
| Chinese Overview | 2933990099. Mimwe mishonga yeheterocyclic ine chete nitrogen heteroatoms.Kukosha-yakawedzerwa mutero wemutero: 17.0%.Mutero wekudzoserwa kwemutero: 13.0%.Regulatory mamiriro: Hapana.Inonyanya kufarirwa nyika mutero: 6.5%.General tariff: 20.0% |
| Declaration elements | Zita rechigadzirwa, ingredient yemukati, shandisa, hexamethylene chloride, ndapota ratidza chitarisiko, 6-caprolactam, ndapota ratidza chitarisiko, kusaina zuva. |
| Summary | 2933990090. heterocyclic compounds nenitrogen hetero-atomu(s) chete.VAT:17.0%.Mutero wekudzoserwa kwemutero: 13.0%..MFN mutero: 6.5%.General tariff:20.0% |
Rumwe ruzivo:
Qu Qiang (PhD muchipatara pharmacology, Dhipatimendi rePharmacy, Xiangya Hospital, Central South University) uye Wang Ruoguang (Chiremba weMishonga, postdoctoral in biology, Changsha Ruoguang Medical Research Center) akanyorawo kuti: muchirongwa che entecavir, entecavir inogona kutorwa. kwemakore akati wandei kana kunyange gumi.Kupfuura makore.Uye inogona kushandiswa nevakadzi vane pamuviri, vachiratidza kuchengeteka kwakanaka.
Tichitarisa kubva kune aya anozivikanwa ma molecular pharmacological mechanisms, Entecavir inogona kuva ne-broad-spectrum antiviral effect, kwete chete inoshanda kurwisana neHBV.
Isu tinowanzo shandisa Entecavir kurapa hutachiona hwehutachiona hwehutachiona mukiriniki, uye mhedzisiro yacho inoshamisa.
Parizvino, mukutarisisa kwevanopfuura mazana mashanu evarwere veCOVID19 muHubei (nzvimbo), munhu mumwe chete akatora entecavir.Nguva yekunyora yaiva kutanga kwaJanuary, uye ipapo mushonga wacho wakamiswa.
Ndichiri kutsigira vashandi vekurapa muHubei, vamwe vanachiremba vepasi, kana mapoka ane njodzi, parizvino ari kushandisa Entecavir kudzivirira COVID19, hapana nyaya yehutachiona.Vanhu vanofungidzirwa kuti vanotora entecavir, hapana akafambira mberi kuti aonekwe aine COVID19.
Patent nyaya:
Iko kune kunyanya maviri maitiro, 06 maitiro uye 89 maitiro.Kupera kwepatent ye06 process kwave kumberi (inopera muna 2023)!Kunyange zvazvo mutengo wekugadzirisa wakaderera, hutano huri hwakanaka, uye vashandi vanogona kuva vakasimba, mazano ega: Pamiti yemakemikari, shandisa nzira ye06 kuti usanyanya kuzvikudza;kumakambani emishonga, usatore fluke uye usanyanya kuve nengozi.
Muna 2014, Chia Tai Tianqing akawana kutengesa kwegore negore kwe 10 bhiriyoni yuan kuburikidza nekuvimba nemishonga yemagetsi yakadai se entecavir, iyo entecavir yakaverengera 20%.
Sezvo entecavir yakabvumirwa kutengeswa muna 2005, kupfuura 100 makambani emishonga epamba akanyorera kunyoreswa kwechigadzirwa;pakati pavo, makambani ekugadzira akatenderwa anosanganisira Jiangsu Zhengda Tianqing Pharmaceutical (yekutanga kutevedzera), Hainan Zhonghe Pharmaceutical, uye Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Pharmaceutical Pharmaceutical, Singchungdong Haing 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, nezvimwewo;kubva pazuva rechibvumirano, chigadzirwa ichi chakapinda mumhando yemhando dzakakurumbira dzakaziviswa kubvira 2007.
JIN DUN Medical aneISO qualification uye inosangana neGMP yekugadzira zviyero, vakashandirwa mudzimba nevekunze nyanzvi dzekugadzira zvinodhaka vane ruzivo rwakapfuma kutungamira R&D yekambani.
TECHNOL OGY ADVANTAGES
●High Pressure Catalytic Hydrogenation .High Pressure Hydrogenolysis Reaction .Cryogenic Reaction (<-78%C)
●Aromatic Heterocyclic Synthesis
● Rearrangement Reaction
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Gignard Reaction
Equipments
Yedu Lab ine midziyo yakasiyana-siyana yekuedza uye yekuedza, yakadai se: 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...
R&D Chikwata
Jindun Medical ine boka revashandi veR&D nyanzvi, uye inoshandisa nyanzvi zhinji dzemumba nedzekunze dzekugadzira zvinodhaka kutungamira R&D, zvichiita kuti kubatanidza kwedu kuve kwakanyatso uye kushanda zvakanaka.
Isu takabatsira akati wandei epamusoro makambani emishonga emishonga, akadaiHansoh, Hengrui uye HEC Pharm.Pano ticharatidza chikamu chavo.
Customization Case One:
Cas Nha.: 110351-94-5
Customization Nyaya Yechipiri:
Cas Nha.: 144848-24-8
Customization Nyaya Yetatu:
Cas Nha.: 200636-54-0
1.Gadzirisa New Intermediates kana maAPI.Zvakangofanana nepamusoro pekugovanisa kesi, vatengi vane zvinodikanwa kune chaiwo maIntermediates kana APIs, uye havagone kuwana zvigadzirwa zvinodikanwa mumusika, saka isu tinogona kubatsira kuGadzirisa.
2.Process Optimization for Old Products.Chikwata chedu chichabatsira Kukwirisa nekuvandudza kugadzirwa kwakadai nzira yemaitiro yasakara, mutengo wekugadzira wakakwira, uye kushanda kwacho kwakadzikira.Tinogona kupa zvizere zvinyorwa zvekufambisa tekinoroji uye kuvandudzwa kwemaitiro, kubatsira mutengi kuti awedzere kugadzirwa.
Kubva pazvinangwa zvezvinodhaka kusvika kuINDs, JIN DUN Medical inokupa iweimwe-stop personalized R&D mhinduro.
JIN DUN Medical inoomerera pakugadzira timu ine zviroto, kugadzira zvigadzirwa zvine chiremera, zvine hungwaru, zvine hungwaru, uye kuenda zvese kunze kuti uve shamwari yakavimbika uye shamwari yevatengi!
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