产品描述
Remdesivir is a nucleoside analogue, with effective antiviral activity( EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells)
体外活性
GS-5734 inhibits murine hepatitis virus (MHV) with similar 50% effective concentration values (EC50) as SARS-CoV and Middle East respiratory syndrome coronavirus (MERS-CoV).?Passage of WT MHV in the presence of the GS-5734 parent nucleoside selected two mutations in the nsp12 polymerase at residues conserved across all CoVs that conferred up to 5.6-fold resistance to GS-5734, as determined by EC50[1].
别名
瑞德西韦;GS-5734;Remdesivir
参考文献
[1]Li Y, Cao L, Li G, et al. Remdesivir Metabolite GS-441524 Efficiently Inhibits SARS-CoV-2 Infection in Mouse Model[J] . Journal of medicinal chemistry. 2020 [2]Silvas J A, Jureka A S, Nicolini A M, et al. Inhibitors of VPS34 and lipid metabolism suppress SARS-CoV-2 replication[J]. bioRxiv. 2020. [3]Agostini M L , Andres E L , Sims A C , et al. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease[J]. Mbio, 2018, 9(2):e00221-18. [4]Wang M , Cao R , Zhang L , et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro[J]. cell research. [5]Nguyenla X, Wehri E, Van Dis E, et al. Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells[J]. bioRxiv. 2020
引用文献
[1]Williams C G, Jureka A S, Silvas J A, et al. Inhibitors of VPS34 and fatty-acid metabolism suppress SARS-CoV-2 replication. Cell Reports. 2021: 109479. [2]Li, Quanjie, et al Corilagin inhibits SARS-CoV-2 replication by targeting viral RNA-dependent RNA polymerase.. Acta Pharmaceutica Sinica B. (2021). [3]Li Y, Cao L, Li G, et al. Remdesivir Metabolite GS-441524 Efficiently Inhibits SARS-CoV-2 Infection in Mouse Model. Journal of Medicinal Chemistry. 2020 [4]Zhao J, Liu Q, Yi D, et al. 5-Iodotubercidin inhibits SARS-CoV-2 RNA synthesis. Antiviral Research. 2022: 105254. [5]Zhao J, Liu Q, Yi D, et al. 5-Iodotubercidin inhibits SARS-CoV-2 RNA synthesis. Antiviral Research. 2022: 105254. [6]Nicholson M W, Huang C Y, Wang J Y, et al. Cardio-and Neurotoxicity of Selected Anti-COVID-19 Drugs. Pharmaceuticals. 2022, 15(6): 765 [7]Nguyenla X, Wehri E, Van Dis E, et al. Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells. Scientific Reports. 2022 Nov 2;12(1):18506.
储存和溶解度
DMSO:125 mg/mL (207.44 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years