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瑞德西韦(1809249-37-3,GS-5734,Remdesivir)属于核苷类似有机化合物,瑞德西韦具有抗病毒的活性,在HAE细胞中可以对SARS-CoV以及MERS-CoVEC50值为 74 nM,在延迟脑肿瘤细胞中,对鼠肝炎病毒的EC50值为30nM。瑞德西韦也是潜在的冠状病毒研究抑制剂,目前已经衍生出的瑞德西韦一磷酸,瑞德西韦二磷酸,瑞德西韦三磷酸等衍生物均是潜在病毒抑制剂,且瑞德西韦三磷酸形式衍生产品对冠状病毒有明显的抑制作用。瑞德西韦在合成过程中存在手性异构体化合物。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
HCY00005-5mg 5mg 98% ¥ 1800.00 ¥ 1800.00 instock
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HCY00005-10mg 10mg 98% ¥ 2800.00 ¥ 2800.00 instock
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HCY00005-50mg 50mg 98% ¥ 5800.00 ¥ 5800.00 instock
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HCY00005-1g 1g 98% ¥ 13800.00 ¥ 13800.00 instock
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中文别名 瑞德沙韦,瑞德西韦(1809249-37-3,GS-5734),瑞德西韦磷酸盐,瑞德西韦异构体,
英文别名 Remdesivir,GS-5734,GS 5734,GS5734,1809249-37-3,
CAS号 1809249-37-3
SMILES CCC(CC)COC(=O)[C@H](C)N[P@](=O)(OC[C@H]1O[C@](C#N)([C@H](O)[C@@H]1O)C1=CC=C2N1N=CN=C2N)OC1=CC=CC=C1
Inchi InChI=1S/C37H48N6O5S2/c1-24(2)33(42-36(46)43(5)20-29-22-49-35(40-29)25(3)4)34(45)39-28(16-26-12-8-6-9-13-26)18-32(44)31(17-27-14-10-7-11-15-27)41-37(47)48-21-30-19-38-23-50-30/h6-15,19,22-25,28,31-33,44H,16-18,20-21H2,1-5H3,(H,39,45)(H,41,47)(H,42,46)/t28-,31-,32-,33-/m0/s1
InchiKey NCDNCNXCDXHOMX-XGKFQTDJSA-N
分子式 Molecular Weight C27H35N6O8P
分子量 Formula 602.2253991
闪点 FP 526.6±34.3 °C
熔点 Melting point NA
沸点 Boiling point 947.0±65.0 °C at 760 mmHg
Polarizability极化度 78.9±0.5 10-24cm3
密度 Density 1.47±0.1 g/cm3(Predicted)
蒸汽压 Vapor Pressure 0.0±0.3 mmHg at 25°C
溶解度Solubility Very slightly soluble inwater,0.339 mg/mL in water; 50 mM in ethano,
性状 固体粉末,Powder
储藏条件 Storage conditions 阴凉干燥处处;Storge at room temperature
瑞德西韦(CAS:1809249-37-3):Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.


Tags:瑞德西韦供应商,Remdesivir,瑞德西韦一磷酸,瑞德西韦二磷酸,瑞德西韦三磷酸,瑞德西韦购买,Remdesivir 瑞德西韦生产,Remdesivir 瑞德西韦 批量,Remdesivir 瑞德西韦 供应,Remdesivir 瑞德西韦 订购,Remdesivir 瑞德西韦采购,瑞德西韦厂家,GS-5734,GS 5734,GS5734,1809249-37-3,Remdesivir,瑞德西韦合成,瑞德西韦的作用,Remdesivir合成原料,Remdesivir中间体
产品说明 瑞德西韦(1809249-37-3,GS-5734 or Remdesivir)是一种病毒抑制剂,瑞德西韦(GS-5734)已经衍生出瑞德西韦一磷酸,瑞德西韦二磷酸,瑞德西韦三磷酸(Remdesivir triphosphate)等衍生物均是潜在病毒抑制剂。
IntroductionRemdesivir, or GS-5734, is an adenosine triphosphate analog first described in the literature in 2016 as a potential treatment for Ebola.1 In 2017, its activity against the coronavirus family of viruses was also demonstrated.2 Remdesivir is also being researched as a potential treatment to SARS-CoV2, the coronavirus responsible for COVID-19.4
Application1潜在冠状病毒抑制剂Experimental Unapproved Treatments for COVID-19
Application2瑞德西韦是一种核苷类似物,用于抑制RNA聚合酶的作用.
Application3瑞德西韦是一种病毒抑制剂,在HAE 细胞中对 MERS-CoV和SARS-CoV的EC50 值均为74 nM,在延迟脑肿瘤细胞中对鼠肝炎病毒的EC50实验值为30nM。A nucleoside analog used to treat RNA virus infections.

Remdesivir或GS-5734是一种三磷酸腺苷类似物,于2016年首次在文献中描述为可能的埃博拉病毒治疗方法.2017年,它还被证明了对冠状病毒家族类病毒的活性有抑制作用。 SARS-CoV-2的潜在治疗方法,冠状病毒负责COVID-19。
Remdesivir, or GS-5734, is an adenosine triphosphate analog first described in the literature in 2016 as a potential treatment for Ebola.In 2017, its activity against the coronavirus family of viruses was also demonstrated.Remdesivir is also being researched as a potential treatment to SARS-CoV-2, the coronavirus responsible for COVID-19.
Remdesivir是一种核苷类似物,有望抑制RNA聚合酶的作用。通过掺入RNA不能添加额外的核苷酸,从而终止RNA转录。已证明RNA聚合酶突变的病毒对remdesivir产生部分抗性传染性较小。
Remdesivir is a nucleoside analog that is expected to inhibit the action of RNA polymerase.By incorporating into RNA, additional nucleotides cannot be added, terminating RNA transcription.Viruses with mutations in RNA polymerase to develop partial resistance to remdesivir have been shown to be less infective.
瑞德西韦研究进展:
1.准备在埃博拉疫情中使用的实验药物
检查海顿E.
国际卫生组织正在与刚果民主共和国讨论如何以及是否采用除疫苗之外的其他疗法。 国际卫生组织正在与刚果民主共和国讨论如何以及是否采用除疫苗之外的其他疗法。 刚果卫生部官员携带了第一批实验性埃博拉疫苗。
2.发现用于治疗埃博拉病毒的药物
Bixler SL,Duplantier AJ,Bavari S.
审查目的:
埃博拉病毒(Filoviridae家族)的成员,是人类严重病毒性出血热的病原体。在过去的40年中,该病毒与非洲几次高死亡率暴发有关,最近在西非暴发导致11,000多人死亡。这篇综述总结了埃博拉病毒病治疗药物的药物发现和开发过程的现状,重点是所使用的策略以及该过程各个阶段面临的挑战。最近发现:尽管有大量的体外功效数据,动物模型中的临床前数据以及人类临床数据,但尚未批准任何疗法可用于治疗埃博拉病毒病。但是,一些有希望的候选人,例如ZMapp和GS-5734,已经进入正在进行的临床试验。

瑞德西韦(GS-5734)在体外有效抑制MERS冠状病毒(MERS-CoV)复制,并在小鼠模型中显示出对严重急性呼吸系统综合症(SARS)-CoV的功效。在这里,我们在MERS-CoV感染的非人类灵长类动物模型恒河猴中测试了预防和治疗性瑞姆昔韦治疗的功效。接种前24小时开始的预防性remdesivir治疗完全预防了MERS-CoV引起的临床疾病,强烈抑制了呼吸系统中MERS-CoV的复制,并防止了肺部病变的形成。接种后12小时开始的雷姆昔韦韦治疗还提供了明显的临床益处,包括临床体征减少,肺部病毒复制减少以及肺部病变的出现和严重程度降低。此处提供的数据支持在MERS临床试验中对雷姆昔韦治疗的疗效进行测试。还可以考虑将其用于更广泛的冠状病毒,包括当前新兴的新型冠状病毒2019-nCoV。


BIOFOUNT公司目前衍生的瑞德西韦产品有:瑞德西韦一磷酸、瑞德西韦二磷酸、瑞德西韦三磷酸、瑞德西韦异构体等形式产品。
警示图
危险性
危险性警示 Data regarding overdoses of remdesivir are not readily available. Overdoses of other nucleoside analogs like acyclovir can be managed with symptomatic and supportive treatment.5
安全声明 NA
安全防护 实验过程防止食如、吸入
备注 NA
瑞德西韦的要用半衰期:在非人类灵长类动物中静脉内剂量为10mg / kg时,血浆半衰期为0.39h。在非人类灵长类动物中,核苷三磷酸代谢物的半衰期为14h。
Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S: Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. [PubMed:26934220]
Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS: Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses. Sci Transl Med. 2017 Jun 28;9(396). pii: 9/396/eaal3653. doi: 10.1126/scitranslmed.aal3653. [PubMed:28659436]
Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR: Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2). pii: mBio.00221-18. doi: 10.1128/mBio.00221-18. [PubMed:29511076]
de Wit E, Feldmann F, Cronin J, Jordan R, Okumura A, Thomas T, Scott D, Cihlar T, Feldmann H: Prophylactic and therapeutic remdesivir (GS-5734) treatment in the rhesus macaque model of MERS-CoV infection. Proc Natl Acad Sci U S A. 2020 Feb 13. pii: 1922083117. doi: 10.1073/pnas.1922083117. [PubMed:32054787]
Vander T, Medvedovsky M, Herishanu Y: Encephalopathy induced by oral acyclovir in a patient with normal renal function. J Infect. 2003 May;46(4):286. doi: 10.1053/jinf.2002.1119. [PubMed:12799156]
  1. Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S: Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 

  2. Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS: Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses. Sci Transl Med. 2017 Jun 28;9(396). pii: 9/396/eaal3653. doi: 10.1126/scitranslmed.aal3653. 

  3. Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR: Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2). pii: mBio.00221-18. doi: 10.1128/mBio.00221-18.

  4. de Wit E, Feldmann F, Cronin J, Jordan R, Okumura A, Thomas T, Scott D, Cihlar T, Feldmann H: Prophylactic and therapeutic remdesivir (GS-5734) treatment in the rhesus macaque model of MERS-CoV infection. Proc Natl Acad Sci U S A. 2020 Feb 13. pii: 1922083117. doi: 10.1073/pnas.1922083117. 

  5. Vander T, Medvedovsky M, Herishanu Y: Encephalopathy induced by oral acyclovir in a patient with normal renal function. J Infect. 2003 May;46(4):286. doi: 10.1053/jinf.2002.1119. 

  6. Ko WC, Rolain JM, Lee NY, Chen PL, Huang CT, Lee PI, Hsueh PR: Arguments in favor of remdesivir for treating SARS-CoV-2 infections. Int J Antimicrob Agents. 2020 Mar 5:105933. doi: 10.1016/j.ijantimicag.2020.105933. 

  7. Grein J, Ohmagari N, Shin D, Diaz G, Asperges E, Castagna A, Feldt T, Green G, Green ML, Lescure FX, Nicastri E, Oda R, Yo K, Quiros-Roldan E, Studemeister A, Redinski J, Ahmed S, Bernett J, Chelliah D, Chen D, Chihara S, Cohen SH, Cunningham J, D'Arminio Monforte A, Ismail S, Kato H, Lapadula G, L'Her E, Maeno T, Majumder S, Massari M, Mora-Rillo M, Mutoh Y, Nguyen D, Verweij E, Zoufaly A, Osinusi AO, DeZure A, Zhao Y, Zhong L, Chokkalingam A, Elboudwarej E, Telep L, Timbs L, Henne I, Sellers S, Cao H, Tan SK, Winterbourne L, Desai P, Mera R, Gaggar A, Myers RP, Brainard DM, Childs R, Flanigan T: Compassionate Use of Remdesivir for Patients with Severe Covid-19. N Engl J Med. 2020 Apr 10. doi: 10.1056/NEJMoa2007016. 

  8. Ledford H: Hopes rise on coronavirus drug remdesivir. Nature. 2020 Apr 29. pii: 10.1038/d41586-020-01295-8. doi: 10.1038/d41586-020-01295-8. 
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