Remdesivir – CAS 1809249-37-3

Description

Remdesivir is a monophosphoramidate prodrug of the C-adenosine nucleoside analogue GS-441524, formed by esterification with 2-ethylbutanol and conjugation to L-alanine phenyl phosphate. Following cellular uptake it is metabolised to the active nucleoside triphosphate, which acts as an alternative substrate for viral RNA-dependent RNA polymerases, causing delayed chain termination. It shows broad-spectrum in vitro antiviral activity against RNA viruses including Ebola virus, MERS-CoV and SARS-CoV, with anti-EBOV EC50 of 86 nM in macrophages, and was evaluated clinically for Ebola virus disease and, in a randomised placebo-controlled trial, for Covid-19, where treated patients had a median recovery time of 10 days. Laboratories use it as a reference antiviral prodrug for RdRp inhibition assays and comparative studies against other nucleotide analogues.

We are also offering active metabolites of Remdesivir: Remdesivir triphosphate, diphosphate or monophosphate.

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References

• Shannon, A.; Le, N. T.-T.; Selisko, B.; Eydoux, C.; Alvarez, K.; Guillemot, J.-C.; Decroly, E.; Peersen, O.; Ferron, F.; Canard, B., Remdesivir and SARS-CoV-2: Structural requirements at both nsp12 RdRp and nsp14 Exonuclease active-sites. Antiviral Res. 2020, 178, 104793.
• Ju, J.; Li, X.; Kumar, S.; Jockusch, S.; Chien, M.; Tao, C.; Morozova, I.; Kalachikov, S.; Kirchdoerfer, R. N.; Russo, J. J., Nucleotide analogues as inhibitors of SARS-CoV polymerase. bioRxiv 2020, 1-18.
• Jordan, P. C.; Liu, C.; Raynaud, P.; Lo, M. K.; Spiropoulou, C. F.; Symons, J. A.; Beigelman, L.; Deval, J., Initiation, extension, and termination of RNA synthesis by a paramyxovirus polymerase. PLoS Pathogens 2018, 14 (2), e1006889/1-e1006889/23.
• Siegel, D.; Hui, H. C.; Doerffler, E.; Clarke, M. O.; Chun, K.; Zhang, L.; Neville, S.; Carra, E.; Lew, W.; Ross, B.; Wang, Q.; Wolfe, L.; Jordan, R.; Soloveva, V.; Knox, J.; Perry, J.; Perron, M.; Stray, K. M.; Barauskas, O.; Feng, J. Y.; Xu, Y.; Lee, G.; Rheingold, A. L.; Ray, A. S.; Bannister, R.; Strickley, R.; Swaminathan, S.; Lee, W. A.; Bavari, S.; Cihlar, T.; Lo, M. K.; Warren, T. K.; Mackman, R. L., 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. J. Med. Chem. 2017, 60 (5), 1648-1661.
• Clarke, M. O. N. H.; Jordan, R.; Mackman, R. L.; Ray, A. S.; Siegel, D. Preparation of amino acid-containing nucleosides for treating flaviviridae virus infections. 2017-US28243, 2017184668, 20170419., 2017.
• Warren, T. K.; Jordan, R.; Lo, M. K.; Ray, A. S.; Mackman, R. L.; Soloveva, V.; Siegel, D.; Perron, M.; Bannister, R.; Hui, H. C.; Larson, N.; Strickley, R.; Wells, J.; Stuthman, K. S.; Van Tongeren, S. A.; Garza, N. L.; Donnelly, G.; Shurtleff, A. C.; Retterer, C. J.; Gharaibeh, D.; Zamani, R.; Kenny, T.; Eaton, B. P.; Grimes, E.; Welch, L. S.; Gomba, L.; Wilhelmsen, C. L.; Nichols, D. K.; Nuss, J. E.; Nagle, E. R.; Kugelman, J. R.; Palacios, G.; Doerffler, E.; Neville, S.; Carra, E.; Clarke, M. O.; Zhang, L.; Lew, W.; Ross, B.; Wang, Q.; Chun, K.; Wolfe, L.; Babusis, D.; Park, Y.; Stray, K. M.; Trancheva, I.; Feng, J. Y.; Barauskas, O.; Xu, Y.; Wong, P.; Braun, M. R.; Flint, M.; McMullan, L. K.; Chen, S.-S.; Fearns, R.; Swaminathan, S.; Mayers, D. L.; Spiropoulou, C. F.; Lee, W. A.; Nichol, S. T.; Cihlar, T.; Bavari, S., Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature (London, United Kingdom) 2016, 531 (7594), 381-385.
• Chun, B. K.; Clarke, M. O. N. H.; Doerffler, E.; Hui, H. C.; Jordan, R.; Mackman, R. L.; Parrish, J. P.; Ray, A. S.; Siegel, D. Preparation of nucleosides and methods for treating Filoviridae virus infections. 2015-14926062 20160122374, 20151029., 2016.
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