GS-441524 (Remdesivir Metabolite)

CHF 65.00
In stock
AG-CR1-3722-M0055 mgCHF 65.00
AG-CR1-3722-M01010 mgCHF 95.00
AG-CR1-3722-M05050 mgCHF 250.00
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Product Details
Product Type Chemical
Properties
Formula

C12H13N5O4

MW 291.3
CAS 1191237-69-0
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (10mg/ml) or DMF (10mg/ml).
Identity Determined by 1H-NMR.
InChi Key BRDWIEOJOWJCLU-LTGWCKQJSA-N
Smiles NC1=NC=NN2C1=CC=C2[C@]3([C@@H]([C@@H]([C@H](O3)CO)O)O)C#N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • GS-441524 is the active prodrug of the broad-spectrum antiviral Remdesivir. GS-441524 is an adenosine nucleotide analog in viral RNA production. It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase and evades proofreading by viral exoribonuclease (ExoN), causing a decrease in viral RNA production (RNA synthesis arrest), either by terminating RNA chains or causing mutations.
  • It inhibits MERS-CoV or SARS-CoV-infected HAE cultures (EC50=74nM and 69nM) and murine hepatitis virus (MHV) (EC50=30nM).
  • In vivo, remdesivir (Prod. No. AG-CR1-3713) (25 and 50 mg/kg) reduces lung viral titers and prevents weight loss in a mouse model of SARS-CoV infection.
  • Remdesivir (Prod. No. AG-CR1-3713) is used as a treatment for Ebola virus disease and Marburg virus infections and other single stranded RNA viruses such as respiratory syncytial virus, Junin virus, Lassa fever virus, Nipah virus, Hendra virus and the coronaviruses (including MERS and SARS viruses).
  • Remdesivir is effective in the control of 2019-nCoV (COVID-19) infection in vitro. It now also has been studied as potential treatment of SARS-CoV-2 infections.
Product References
  1. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys: T.K. Warren, et al.; Nature 531, 381 (2016)
  2. Late Ebola virus relapse causing meningoencephalitis: a case report: M. Jacobs, et al.; Lancet 388, 498 (2016)
  3. Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses: T.P. Sheahan, et al.; Sci. Transl. Med. 9, eaal3653 (2017)
  4. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses; D. Siegel, et al.; J. Med. Chem. 60, 1648 (2017)
  5. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease: M.L. Agostini, et al.; mBio 9, e00221 (2018)
  6. Mechanism of Inhibition of Ebola Virus RNA-Dependent RNA Polymerase by Remdesivir: E.P. Tchesnokov, et al.; Viruses 11, E326 (2019)
  7. Remdesivir (GS-5734) protects African green monkeys from Nipah virus challenge: M.K. Lo, et al.; Sci. Transl. Med. 11, eaau9242 (2019)
  8. Broad spectrum antiviral remdesivir inhibits human endemic and zoonotic deltacoronaviruses with a highly divergent RNA dependent RNA polymerase: A.J. Brown, et al.; Antiviral Res. 169, 104541 (2019)
  9. Prophylactic and therapeutic remdesivir (GS-5734) treatment in the rhesus macaque model of MERS-CoV infection: R. de Wit, et al.; PNAS (Epub ahead of print) (2020)
  10. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro: M. Wang, et al.; Cell Res. 30, 269 (2020)
  11. Comparative therapeutic efficacy of remdesivir and combination lopinavir, ritonavir, and interferon beta against MERS-CoV: T.P. Sheahan, et al.; Nat. Commun. 11, 222 (2020)
  12. The antiviral compound remdesivir potently inhibits RNA-dependent RNA polymerase from Middle East respiratory syndrome coronavirus: C.J. Gordon, et al.; J. Biol. Chem. (Epub ahead of print) (2020)
  13. Arguments in favour of remdesivir for treating SARS-CoV-2 infections: W.C. Ko, et al.; Int. J. Antimicrob. Agents (Epub ahead of print) (2020)
  14. Remdesivir triphosphate blocks DNA synthesis and increases exonucleolysis by the replicative mitochondrial DNA polymerase, Pol γ: E.J. Ciesielska, et al.; Mitochondrion 61, 147 (2021)
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