Entecavir (SQ 34676;BMS 200475) zaɓi ne kuma mai hana HBV mai inganci.A cikin sel HepG2 EC50 darajar 3.75 nM.Sabbin magungunan anti-hepatitis B da magungunan kanjamau na farko.
Entecavir sakamako
Wannan samfurin shine analog na guanine nucleoside, wanda ke da tasirin hanawa akan cutar hanta B (HBV) polymerase.Ana iya sanya shi cikin phosphorylated cikin triphosphate mai aiki, kuma rabin rayuwar triphosphate a cikin tantanin halitta shine sa'o'i 15.Ta hanyar yin gasa tare da HBV polymerase's na halitta substrate deoxyguanosine triphosphate, entecavir triphosphate na iya hana duk ayyuka uku na kwayar cutar polymerase (reverse transcriptase): (1) HBV polymerase farawa;(2) pregenomic mRNA Samuwar madaidaicin madaidaicin rubutun baya;(3) Haɗin ingantacciyar igiyar HBV DNA.Tsawon inhibitory (Ki) na entecavir triphosphate akan HBV DNA polymerase shine 0.0012μM.Entecavir triphosphate yana da tasirin hanawa mai rauni akan tantanin halitta α, β, δ DNA polymerase da mitochondrial γ DNA polymerase, tare da ƙimar Ki na 18 zuwa 160 μM.
Bayyana | Entecavir (SQ 34676;BMS 200475) zaɓi ne kuma mai tasiri HBV Inhibitor. A cikin sel HepG2 EC50 darajar 3.75 nM. |
Masu alaƙasassa | Hanyar sigina >> Anti-infective >> HBV Bincike wuraren >> Kamuwa da cuta |
manufa | EC50: 3.75 nM (anti-HBV, HepG2 cell)[2] |
In vitrokaratu | EC50 na BMS-200475 zuwa HBV shine 3.75 nM.An shigar da shi cikin furotin na HBV, sannan an hana matakin farawa na juyar da rubutun.Ayyukan antiviral na BMS-200475 yana da ƙasa da ƙasa fiye da sauran ƙwayoyin RNA da DNA [1].Idan aka kwatanta da sauran analogues deoxyguanosine (penciclovir, ganciclovir, lobucavir da acyclovir) ko lamivudine, entecavir zai iya zama phosphorylated zuwa metabolite mai aiki.Rabin rayuwar cikin salula na Entecavir shine sa'o'i 15 [2]. |
A cikin vivobincike | BMS-200475 ana bi da shi ta baki kowace rana tare da kashi daga 0.02 zuwa 0.5 MG / kg nauyin jiki na tsawon watanni 1 zuwa 3, wanda zai iya rage girman ƙwayar cutar hanta ta woodchuck (WHV) a cikin katako mai ciwon daji na kullum [3]. |
Cellgwaji | An shirya BMS 200475 a cikin phosphate buffered saline (PBS) kuma an diluted tare da matsakaicin matsakaici mai ɗauke da 2% fetal bovine serum.Kwayoyin HepG2 2.2.15 an shuka su a kan faranti mai rufi na 12 mai kyau Biocoat collagen a yawan 5 × 10 5 sel a kowace rijiya, kuma an adana su a cikin yanayi mai rikitarwa don kwanaki 2 zuwa 3, sannan an rufe shi da 1 ml na BMS 200475 matsakaici .An yi kididdigar HBV a rana ta 10 [1]. |
Magana | [1].Inamo SF, et al.Gano BMS-200475 a matsayin mai ƙarfi da zaɓi mai hana cutar hepatitis B.Magungunan Antimicrob Agents Chemother.1997 Jul; 41 (7): 1444-9.[2].Rivkin A, et al.Bita na entecavir a cikin maganin ciwon hanta na kullum.Curr Med Res Ra'ayin.2005 Nov; 21 (11): 1845-57.[3].Genovesi EV, et al.Ingancin Carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 a cikin samfurin woodchuck na kamuwa da cutar hanta B.Magungunan Antimicrob Agents Chemother.1998 Dec; 42 (12): 3209-18. |
Halin jiki da sinadarai na Entecavir
Yawan yawa | 1.8 ± 0.1 g/cm3 |
Wurin tafasa | 734.2ºC a 760 mmHg |
Wurin narkewa | 249-252ºC |
Tsarin kwayoyin halitta | Saukewa: C12H15N5O3 |
Nauyin kwayoyin halitta | 277.279 |
Wurin walƙiya | 397.9ºC |
Daidaitaccen inganci | 277.117493 |
PSA | 130.05000 |
LogP | -0.96 |
Halayen bayyanar | Fari zuwa fari-fari/rawaya crystalline foda |
Indexididdigar refractive | 1.837 |
Yanayin ajiya | -20°C injin daskarewa |
Entecavir Kwastam
Lambar kwastam | 293399009 |
Bayanin Sinanci | 2933990099. Sauran mahadi heterocyclic dauke da nitrogen heteroatoms kawai.Ƙimar-Ƙara haraji: 17.0%.Yawan rangwamen haraji: 13.0%.Sharuɗɗan tsari: Babu.Farashin kuɗin ƙasa mafi fifiko: 6.5%.Janar jadawalin kuɗin fito: 20.0% |
Abubuwan sanarwa | Sunan samfur, abun ciki na sinadarai, amfani, hexamethylene chloride, da fatan za a nuna bayyanar, 6-caprolactam, da fatan za a nuna bayyanar, ranar sa hannu |
Takaitawa | 2933990090. heterocyclic mahadi tare da nitrogen hetero-atom(s) kawai.VAT: 17.0%.Yawan rangwamen haraji: 13.0%..Farashin MFN: 6.5%.Janar jadawalin kuɗin fito: 20.0% |
Ƙarin bayani:
Qu Qiang (PhD a fannin likitanci na asibiti, Sashen Magunguna, Asibitin Xiangya, Jami'ar Kudancin Kudancin) da Wang Ruoguang (Doctor of Medicine, postdoctoral in Biology, Changsha Ruoguang Medical Center) ya kuma rubuta cewa: a cikin tsarin entecavir, ana iya ɗaukar entecavir. shekaru da yawa ko ma shekaru 10.Fiye da shekaru.Kuma mata masu juna biyu za su iya amfani da shi, yana nuna aminci mai kyau.
Yin la'akari da waɗannan sanannun hanyoyin magunguna na ƙwayoyin cuta, Entecavir na iya samun tasirin antiviral mai faɗi, ba kawai tasiri akan HBV ba.
Har ila yau, sau da yawa muna amfani da Entecavir don magance cututtuka na numfashi na hoto a cikin asibiti, kuma tasirin yana da ban mamaki.
A halin yanzu, a cikin bincike na baya-bayan nan na sama da 500 COVID19 marasa lafiya a Hubei (wani wuri), mutum ɗaya ne kawai ya ɗauki entecavir.Lokacin rubuta magani ya kasance a farkon watan Janairu, sannan aka dakatar da maganin.
Yayin tallafawa ma'aikatan kiwon lafiya a Hubei, wasu likitocin asali, ko ƙungiyoyi masu haɗari, a halin yanzu suna amfani da Entecavir don hana COVID19, babu wani kamuwa da cuta.Mutanen da ake zargi suna shan entecavir, babu wanda ya sami ci gaba don kamuwa da cutar ta COVID19.
Matsalolin haƙƙin mallaka:
Akwai galibi matakai guda biyu, 06 tsari da tsari 89.Ƙarewar takardar shaidar don tsarin 06 ya yi da wuri (zai ƙare a 2023)!Kodayake farashin tsarin yana da ƙasa, ingancin yana da kyau, kuma ma'aikata na iya zama masu karfi, shawarwari na sirri: Don tsire-tsire masu sinadaran, yi amfani da tsarin 06 don kada ku kasance masu girman kai;ga kamfanonin harhada magunguna, kada ku yi tagumi kuma kada ku kasance masu haɗari sosai.
A shekarar 2014, Chia Tai Tianqing ya samu cinikin yuan biliyan 10 a duk shekara ta hanyar dogaro da magunguna iri-iri kamar su entecavir, wanda entecavir ya kai kashi 20%.
Tun lokacin da aka amince da entecavir don shigo da kaya a cikin 2005, fiye da kamfanonin magunguna na cikin gida 100 sun nemi rajistar samfurin;Daga cikin su, kamfanonin da aka amince da su sun hada da Jiangsu Zhengda Tianqing Pharmaceutical (kwaikwayi na farko), Hainan Zhonghe Pharmaceutical, da Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical Pharmaceutical Shanghai, Suzhou Dawnrays Pharmaceutical Pharmaceutical Hainan. kautical, Shandong 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, da dai sauransu.;kara daga kwanan wata kwangila, wannan samfurin ya shiga cikin sahu na rare ayyana iri tun 2007.
JIN DUN Medical yaCancantar ISO kuma ya cika ka'idodin samar da GMP, ƙwararrun ƙwararrun haɗaɗɗun ƙwayoyi na cikin gida da na waje tare da ƙwararrun ƙwarewa don jagorantar R&D na kamfani.
TECHNOL OGY AMFANIN
●High Matsi Catalytic Hydrogenation.Babban Matsi na Hydrogenolysis Reaction.Maganin Cryogenic (<-78% C)
●Aromatic Heterocyclic Synthesis
●Maganar Sake Shiryawa
●Matsalar Chiral
●Heck, Suzuki,Negishi,Sonogashira .Gignard Reaction
Kayan aiki
Our Lab yana da daban-daban na gwaji da kuma gwaji kayan aiki, kamar: NMR (Bruker 400M), HPC, Chiral-HPLC, LC-MS, LC-MS/MS (API 4000) , IR, UV, GC, GC-MS, Chromatography, Microwave Synthesizer, Parallel Synthesizer, Bambance-bambancen Scanning Calorimeter (DSC), Electron Microscope...
Ƙungiyar R&D
Jindun Medical yana da rukuni na ƙwararrun ma'aikatan R&D, kuma yana ɗaukar ƙwararrun masana harhada magunguna na cikin gida da na waje don jagorantar R&D, yana sa ƙirarmu ta fi dacewa da inganci.
Mun taimaka wa manyan kamfanonin harhada magunguna na cikin gida da yawa, kamarHansoh, Hengrui da HEC Pharm.Anan zamu nuna sashinsu.
Hali na Farko na Farko:
Lambar Waya: 110351-94-5
Hali na Musamman na Biyu:
Lambar Waya: 144848-24-8
Halin Hali na Uku:
Lambar Waya: 200636-54-0
1.Keɓance Sabbin Matsakaici ko APIs.Daidai da raba shari'ar na sama, abokan ciniki suna da buƙatun takamaiman Matsakaici ko APIs, kuma ba za su iya samun samfuran da ake buƙata ba a kasuwa, sannan za mu iya taimakawa don Keɓancewa.
2.Haɓaka Tsari don Tsofaffin Kayayyaki.Ƙungiyarmu za ta taimaka don ingantawa da haɓaka irin wannan samarwa wanda hanyar amsawa ta tsufa, farashin samarwa yana da yawa, kuma ingancin ya yi ƙasa.Za mu iya samar da cikakkun takardun shaida don canja wurin fasaha da haɓaka tsari, taimakawa abokin ciniki don samar da ingantaccen aiki.
Daga maƙasudin miyagun ƙwayoyi zuwa INDs, JIN DUN Medical yana ba kumafita na R&D keɓaɓɓen tsayawa ɗaya tasha.
JIN DUN Medical ya dage kan ƙirƙirar ƙungiyar tare da mafarkai, yin samfura masu daraja, ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwararrun ƙwaƙƙwaran, masu tsattsauran ra'ayoyi, masu tsauri, da kuma fita gabaɗaya don zama amintaccen abokin tarayya kuma abokin abokan ciniki!