GS‐441524
A nucleotide analogue.
General information
GS-441524 is an adenine nucleotide analogue similar to remdesivir. It has shown efficacy in Feline Infectious Peritonitis treatment (DrugBank). GS-441524 is also a metabolite of remdesivir (ChEBI).
GS-441524 on PubChem
GS-441524 on Wikipedia
Synonyms
(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile; GS441524
C1=C2C(=NC=NN2C(=C1)[C@]3([C@@H]([C@@H]([C@H](O3)CO)O)O)C#N)N
Supporting references
| Link | Tested on | Impact factor | Notes | Publication date |
|---|---|---|---|---|
|
In vitro activity of itraconazole against SARS‐CoV‐2
Small molecule In vitro |
Caco‐2 cells; VeroE6‐eGFP cells; SARS-CoV-2 strain hCoV-19/Germany/FrankfurtFFM1/2020; SARS-CoV-2 strain BetaCov/Belgium/GHB-03021/2020 | 2.02 | At 3.7 μM, the compound reduced SARS-CoV-2 RNA loads in VeroE6-eGFP cells by more than 4 orders of magnitude. |
Mar/05/2021 |
|
The preclinical inhibitor GS441524 in combination with GC376 efficaciously inhibited the proliferation of SARS-CoV-2 in the mouse respiratory tract
RdRpol Crystallization Small molecule Animal model In vitro |
crystallization; Vero E6 cells; Sprague Dawley rats (pharmacokinetics only); specific pathogen-free mice (toxicity); BALB/c mice; mouse-adapted SARS-CoV-2 (HRB26M); SARS-CoV-2 (HRB26) | 5.78 | The compound was not cytotoxic. The compound inhibited SARS-CoV-2 with an EC50 of ca. 5.188 μM or 5.047 μM in Vero E6 cells for a human and a mouse-adapted version, respectively. Combined with GC376 the values were ca. 0.531 μM and 0.369 μM, respectively. Synergistic effect was also observed in mice after a viral challenge (protection of mice against viral replication in upper and lower respiratory tract) and co-administration of the drugs is supported by pharmacokinetics observations. GS-441524 administered alone was efficacious, as well, though. Combined intranasal and intramuscular routes of administration showed good inhibitory profile. |
Mar/19/2021 |
