Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Remdesivir [1809249-37-3]
Cat# T7766-1mL
Size : 1mL
Brand : TargetMol
Remdesivir
Catalog No. T7766 CAS 1809249-37-3
Synonyms: GS-5734
Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19.
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Remdesivir, CAS 1809249-37-3
| Description | Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19. |
| Targets&IC50 | SARS-CoV:74 nM (EC50) , MERS-CoV:74 nM (EC50) |
| In vitro | METHODS: Mouse hepatitis virus (MHV)-infected DBT cells were incubated with Remdesivir (0.01-1 µM) for 24 h, and the supernatant was analyzed for viral titer by plaque assay. RESULTS: Remdesivir effectively inhibited MHV with an EC50 of 0.03 µM. [1] METHODS: 2019-nCoV-infected Vero E6 cells were treated with Remdesivir (0-400 µM) for 48 h. Viral yield in cell supernatants was detected using qRT-PCR. RESULTS: Remdesivir effectively blocked viral infection at low micromolar concentrations and showed high SI (EC50 = 0.77 μM; CC50 > 100 μM; SI > 129.87). [2] |
| In vivo | METHODS: To assay antiviral activity in vivo, Remdesivir (25 mg/kg, 12% sulfobutylether-β-cyclodextrin sodium salt in water (with HCl/NaOH) at pH 5.0) was injected subcutaneously into MERS-CoV-infected Ces1c-/- hDPP4 mice twice daily. RESULTS: Prophylactic Remdesivir reduced MERS-CoV replication and disease. [3] METHODS: To assay antiviral activity in vivo, Remdesivir (25 mg/kg once daily, administered three times) and Loratadine (10 mg/kg once daily, administered four times) were administered intraperitoneally to 501Y.V2 SARS-CoV-2 infected BALB/c mice. RESULTS: The combination of Remdesivir and the antihistamine Loratadine reduced SARS-CoV-2 replication and inflammation and protected against lung injury. [4] |
| Synonyms | GS-5734 |
| Molecular Weight | 602.58 |
| Formula | C27H35N6O8P |
| CAS No. | 1809249-37-3 |
Storage
Solubility Information
DMSO: 50 mg/mL (82.98 mM)
References and Literature
1. Agostini ML, et al. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2):e00221-18. 2. Wang M, et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro. Cell Res. 2020 Mar;30(3):269-271. 3. Sheahan TP, et al. Comparative therapeutic efficacy of remdesivir and combination lopinavir, ritonavir, and interferon beta against MERS-CoV. Nat Commun. 2020 Jan 10;11(1):222. 4. Wu ML, et al. Combinational benefit of antihistamines and remdesivir for reducing SARS-CoV-2 replication and alleviating inflammation-induced lung injury in mice. Zool Res. 2022 May 18;43(3):457-468. 5. 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
Citations
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. 8. Yousefi M, Lee W S, Chan W O Y, et al.Betacoronaviruses SARS-CoV-2 and HCoV-OC43 Infections in IGROV-1 Cell Line Require Aryl Hydrocarbon Receptor.Emerging Microbes & Infections.2023 (just-accepted): 2256416. 9. Chen Y, Guo Y, Li S, et al.Remdesivir inhibits the progression of glioblastoma by enhancing endoplasmic reticulum stress.Biomedicine & Pharmacotherapy.2023, 157: 114037. 10. Leng L, Xu Z, Hong B, et al.Cepharanthine analogs mining and genomes of Stephania accelerate anti-coronavirus drug discovery.Nature Communications.2024, 15(1): 1537.