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) jẹ yiyan ati imunadoko HBV Inhibitor.Ninu awọn sẹẹli HepG2 iye EC50 jẹ 3.75 nM.Awọn egboogi-jedojedo B tuntun ati awọn oogun laini akọkọ ti egboogi-AIDS.
Entecavir ipa
Ọja yii jẹ afọwọṣe guanine nucleoside, eyiti o ni ipa inhibitory lori ọlọjẹ jedojedo B (HBV) polymerase.O le jẹ phosphorylated sinu triphosphate ti nṣiṣe lọwọ, ati idaji-aye ti triphosphate ninu sẹẹli jẹ wakati 15.Nipa jije pẹlu HBV polymerase's adayeba sobusitireti deoxyguanosine triphosphate, entecavir triphosphate le dojuti gbogbo awọn iṣẹ mẹta ti polymerase gbogun ti (iyipada transcriptase): (1) Ibẹrẹ HBV polymerase;(2) mRNA pregenomic Ibiyi ti okun odi ti transcription yiyipada;(3) Akopọ ti okun rere ti HBV DNA.Igbagbogbo inhibitory (Ki) ti entecavir triphosphate lori HBV DNA polymerase jẹ 0.0012μM.Entecavir triphosphate ni ipa inhibitory alailagbara lori sẹẹli α, β, δ DNA polymerase ati mitochondrial γ DNA polymerase, pẹlu iye Ki ti 18 si 160 μM.
| Apejuwe | Entecavir (SQ 34676;BMS 200475) jẹ yiyan ati imunadoko HBV Inhibitor.Ninu awọn sẹẹli HepG2 EC50 iye jẹ 3.75 nM. |
| Jẹmọisori | Ona ifihan agbara >> Anti-active >> HBV Awọn agbegbe Iwadi >> Arun |
| Àfojúsùn | EC50: 3.75 nM (egboogi-HBV, sẹẹli HepG2)[2] |
| Ninu fitiroawọn ẹkọ | EC50 ti BMS-200475 si HBV jẹ 3.75 nM.O ti dapọ si awọn alakoko amuaradagba HBV, ati lẹhinna igbesẹ ibẹrẹ ti yiyipada transcriptase jẹ idinamọ.Iṣẹ ṣiṣe antiviral ti BMS-200475 kere pupọ ju RNA ati awọn ọlọjẹ DNA miiran [1].Ti a bawe pẹlu awọn analogues deoxyguanosine miiran (penciclovir, ganciclovir, lobucavir ati acyclovir) tabi lamivudine, entecavir jẹ diẹ sii lati jẹ phosphorylated si metabolite ti nṣiṣe lọwọ.Igbesi aye idaji inu sẹẹli ti Entecavir jẹ wakati 15 [2]. |
| Ni vivoiwadi | BMS-200475 ni a tọju ni ẹnu lojoojumọ pẹlu iwọn lilo lati 0.02 si 0.5 mg / kg iwuwo ara fun oṣu 1 si 3, eyiti o le dinku ipele ti kokoro jedojedo woodchuck (WHV) viremia ni imunadoko ni awọn woodchucks onibaje [3]. |
| Ẹyin sẹẹliṣàdánwò | BMS 200475 ti wa ni pese sile ni fosifeti buffered saline (PBS) ati ti fomi po pẹlu ohun yẹ alabọde ti o ni 2% oyun omi ara bovine.Awọn sẹẹli HepG2 2.2.15 ti wa ni irugbin lori awo 12-daradara Biocoat collagen ti a bo ni iwuwo ti awọn sẹẹli 5 × 10 5 fun kanga kan, ati pe a tọju ni ipo idapọ fun awọn ọjọ 2 si 3, ati lẹhinna bo pelu 1 mL ti BMS 200475 alabọde .Iwọn HBV ni a ṣe ni ọjọ 10th [1]. |
| Awọn itọkasi | [1].Innaimo SF, et al.Idanimọ ti BMS-200475 bi agbara ati oludena yiyan ti ọlọjẹ jedojedo B.Awọn aṣoju Antimicrob Chemother.1997 Jul; 41 (7): 1444-9.[2].Rivkin A, et al.Atunwo ti entecavir ni itọju ti arun jedojedo B onibaje.Curr Med Res Opin.2005 Oṣu kọkanla; 21 (11): 1845-57. [3].Genovesi EV, et al.Agbara ti carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 ninu awoṣe woodchuck ti kokoro arun jedojedo B.Awọn aṣoju Antimicrob Chemother.1998 Oṣu kejila; 42 (12): 3209-18. |
Awọn ohun-ini ti ara ati kemikali ti Entecavir
| iwuwo | 1,8 ± 0,1 g / cm3 |
| Oju omi farabale | 734.2ºC ni 760 mmHg |
| Ojuami yo | 249-252ºC |
| Ilana molikula | C12H15N5O3 |
| Ìwúwo molikula | 277.279 |
| oju filaṣi | 397.9ºC |
| Didara to peye | 277.117493 |
| PSA | 130.05000 |
| LogP | -0.96 |
| Awọn ami ifarahan | Funfun si pa-funfun/ofeefee kristali lulú |
| Atọka itọka | 1.837 |
| Awọn ipo ipamọ | -20°C firisa |
Awọn kọsitọmu Entecavir
| koodu kọsitọmu | 2933990099 |
| Chinese Akopọ | 2933990099. Awọn agbo ogun heterocyclic miiran ti o ni awọn heteroatoms nitrogen nikan.Oṣuwọn owo-ori ti a ṣafikun: 17.0%.Oṣuwọn idinku owo-ori: 13.0%.Awọn ipo ilana: Ko si.Owo-ori orilẹ-ede ti o ni ojurere julọ: 6.5%.Owo idiyele gbogbogbo: 20.0% |
| Awọn eroja ikede | Orukọ ọja, akoonu eroja, lilo, hexamethylene kiloraidi, jọwọ tọkasi irisi, 6-caprolactam, jọwọ tọkasi ifarahan, ọjọ iforukọsilẹ |
| Lakotan | 2933990090. awọn agbo ogun heterocyclic pẹlu nitrogen hetero-atom(s) nikan.VAT: 17.0%.Oṣuwọn idinku owo-ori: 13.0%..Owo idiyele MFN: 6.5%.Owo idiyele gbogbogbo: 20.0% |
Alaye ni Afikun:
Qu Qiang (PhD ni ile-iwosan oogun, Sakaani ti Ile elegbogi, Ile-iwosan Xiangya, Ile-ẹkọ giga Central South) ati Wang Ruoguang (Dokita ti Isegun, postdoctoral ni isedale, Ile-iṣẹ Iwadi Iṣoogun Changsha Ruoguang) tun kọwe pe: ninu ilana entecavir, entecavir le ṣee mu. fun opolopo odun tabi paapa 10 ọdun.Diẹ ẹ sii ju ọdun lọ.Ati pe o le ṣee lo nipasẹ awọn aboyun, fifi aabo to dara han.
Ni idajọ lati awọn ilana elegbogi molikula ti a mọ, Entecavir le ni ipa antiviral ti o gbooro, kii ṣe munadoko nikan lodi si HBV.
A tun lo Entecavir nigbagbogbo lati tọju awọn akoran atẹgun ti gbogun ti ni ile-iwosan, ati pe ipa naa jẹ iyalẹnu.
Ni lọwọlọwọ, ni atunyẹwo ifẹhinti ti diẹ sii ju awọn alaisan COVID19 500 ni Hubei (ibi kan), eniyan kan ṣoṣo ni o mu entecavir.Akoko oogun ni ibẹrẹ Oṣu Kini, lẹhinna a da oogun naa duro.
Lakoko ti o ṣe atilẹyin oṣiṣẹ iṣoogun ni Hubei, diẹ ninu awọn dokita koriko, tabi awọn ẹgbẹ eewu giga, lọwọlọwọ nlo Entecavir lati ṣe idiwọ COVID19, ko si ọran ti ikolu.Awọn eniyan ti a fura si mu entecavir, ko si ẹnikan ti o ni ilọsiwaju lati ṣe ayẹwo pẹlu COVID19.
Awọn oran itọsi:
Awọn ilana meji wa ni akọkọ, ilana 06 ati ilana 89.Ipari ti itọsi fun ilana 06 ti wa ni kutukutu (pari ni 2023)!Botilẹjẹpe idiyele ilana naa jẹ kekere, didara dara dara, ati pe awọn oṣiṣẹ le lagbara, imọran ti ara ẹni: Fun awọn ohun ọgbin kemikali, lo ilana 06 lati ma ṣe igberaga pupọ;fun awọn ile-iṣẹ elegbogi, maṣe gba ijakadi ati maṣe ni eewu pupọ.
Ni ọdun 2014, Chia Tai Tianqing ṣaṣeyọri awọn tita ọja lododun ti 10 bilionu yuan nipa gbigbekele awọn oogun jeneriki gẹgẹbi entecavir, eyiti entecavir ṣe iṣiro fun 20%.
Niwọn igba ti a fọwọsi entecavir fun gbigbe wọle ni ọdun 2005, diẹ sii ju awọn ile-iṣẹ oogun ile 100 ti lo fun iforukọsilẹ ọja naa;laarin wọn, awọn ile-iṣẹ iṣelọpọ ti a fọwọsi pẹlu Jiangsu Zhengda Tianqing Pharmaceutical (afarawe akọkọ), Hainan Zhonghe Pharmaceutical, ati Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical Pharmaceutical Shanghai, Suzhou Dawnrays Pharmaceutical ceutical, 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, ati bẹbẹ lọ;siwaju lati ọjọ ti adehun, ọja yii ti wọ awọn ipo ti awọn oriṣi ikede olokiki lati ọdun 2007.
JIN DUN Medical niIjẹrisi ISO ati pade awọn iṣedede iṣelọpọ GMP, oojọ ti abele ati ajeji oogun kolaginni amoye pẹlu ọlọrọ iriri lati dari R&D ile-iṣẹ.
TECHNOL OGY anfani
● Giga titẹ agbara ti o ni itọsi hydrogenation.Iṣeduro Hydrogenolysis Ipa giga.Idahun Cryogenic (<-78%C)
●Aromatic Heterocyclic Synthesis
● Iṣe atunṣe
● Ipinnu Chiral
●Hekki, Suzuki,Negishi,Sonogashira .Gignard lenu
Awọn ohun elo
Lab wa ni orisirisi awọn ohun elo idanwo ati awọn ohun elo idanwo, gẹgẹbi: NMR (Bruker 400M), HPLC, Chiral-HPLC, LC-MS, LC-MS/MS (API 4000) Makirowefu Synthesizer, Parallel Synthesizer, Iyatọ Ṣiṣayẹwo Calorimeter (DSC), Maikirosikopu Electron...
R&D Egbe
Jindun Medical ni ẹgbẹ kan ti oṣiṣẹ R&D alamọdaju, o si gba ọpọlọpọ awọn amoye iṣelọpọ oogun ti ile ati ajeji lati ṣe itọsọna R&D, ṣiṣe iṣelọpọ wa ni deede ati daradara.
A ti ṣe iranlọwọ fun ọpọlọpọ awọn ile-iṣẹ elegbogi inu ile, biiHansoh, Hengrui ati HEC Pharm.Nibi a yoo ṣe afihan apakan ninu wọn.
Ọran Isọdi Ọkan:
Cas No.: 110351-94-5
Isọdi Isọdi Meji:
Cas No.: 144848-24-8
Ọran Isọdọtun Mẹta:
Cas No.: 200636-54-0
1.Ṣe akanṣe Awọn agbedemeji Tuntun tabi APIs.Kanna gẹgẹbi pinpin ọran loke, awọn alabara ni awọn ibeere fun Awọn agbedemeji kan pato tabi awọn API, ati pe wọn ko le rii awọn ọja ti o nilo ni ọja, lẹhinna a le ṣe iranlọwọ lati Ṣe akanṣe.
2.Imudara ilana fun Awọn ọja atijọ.Ẹgbẹ wa yoo ṣe iranlọwọ lati mu ki o mu iru iṣelọpọ pọ si ti ipa ọna iṣe rẹ jẹ arugbo, idiyele iṣelọpọ ga, ati ṣiṣe jẹ kekere.A le pese iwe kikun fun gbigbe imọ-ẹrọ ati ilọsiwaju ilana, iranlọwọ alabara fun iṣelọpọ ti o munadoko diẹ sii.
Lati awọn ibi-afẹde oogun si awọn IND, Iṣoogun JIN DUN pese fun ọawọn solusan R&D ti ara ẹni iduro-ọkan.
Iṣoogun JIN DUN tẹnumọ lori ṣiṣẹda ẹgbẹ kan pẹlu awọn ala, ṣiṣe awọn ọja ti o ni ọlá, titọ, lile, ati lilọ gbogbo jade lati jẹ alabaṣepọ ti o gbẹkẹle ati ọrẹ awọn alabara!
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