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Chemical Structure| 1191237-69-0 Chemical Structure| 1191237-69-0

Structure of GS-441524
CAS No.: 1191237-69-0

Chemical Structure| 1191237-69-0

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GS-441524 is the major active metabolite of Remdesivir, exhibiting superior activity compared to Remdesivir. In primary human lung and cat cell models infected with the virus, GS-441524 shows similar activity with an EC50 value of 0.78 μM against feline infectious peritonitis virus (FIPV).

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Aidan J. Mulligan ; Megan E. Browning ;

Abstract: OBJECTIVE: Feline infectious peritonitis is fatal, and due to lack of approved treatments, unregulated antiviral drugs are used to treat this disease. This study set out to determine the purity of various batches of these drugs from several companies, characterize them, and note any impurities or other unusual characteristics. We also developed a method to qualitatively assess the primary components before administration. SAMPLES: We tested 30 vials from 17 brands of GS-441524 and 5 vials from 1 brand of GC376. We compared the GS-441524 to a control standard from Ambeed and the GC376 to a standard from Cayman Chemical. METHODS: We recorded physical appearance, pH, absorbance, HPLC retention times, and thin-layer chromatography retention factors for all of the samples. Some samples were used for nuclear magnetic resonance and mass spectrometric analysis. RESULTS: Some of the GS-441524 vials were 10% to 25% more concentrated than advertised, but most of the GS-441524 samples tested were similar in purity and composition, both between batches and between brands. We also tested 5 vials of GC376 and found that 1 of the 5 vials contained GS-441524 rather than GC376 and the other 4 vials contained molnupiravir. CLINICAL RELEVANCE: While all of the GS-441524 vials contained GS-441524, none of the GC376 vials tested contained GC376. GC376 is used in cats that are unresponsive to GS-441524, and use of the wrong antiviral can cause serious side effects. We provide suggested methods for distinguishing one drug from the other in new batches.

Keywords: coronavirus ; FIP ; GS-441524 ; GC376 ; molnupiravir

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Aidan J. Mulligan ; Megan E. Browning ;

Abstract: Background: Feline Infectious peritonitis (FlP) is a disease caused by feline coronavirus. FlP is100% fatal and was considered untreatable until recently. Although there is no FDA-approved treatment for FlP, experimental drugs, GS-441524 (the primary metabolite ofremdesivir), GC376 (a viral protease inhibitor), and Molnupiravir have been foundeffective in treating this otherwise fatal disease. Because of the severity of FlP and lackof approved treatments, these drugs are sometimes used off-label to treat this diseaseThese drugs can be obtained through crowdsource online social media groups. Methods: We tested 28 vials from 10 brands of GS-441524 and 5 vials from one brand of GC376We compared the GS-441524 to a control standard from Ambeed and the GC376 to astandard from Cayman Chemical. We recorded physical appearance, pH, absorbance.high-performance liquid chromatography retention times, and thin-layer chromatographyretention factors for all of them. Some were also used for nuclear magnetic resonanceand mass spectrometric analysis. Objectives: These medications are unregulated, and therefore come with potential risks for animalsbeing treated. This study set out to determine the purity of various batches of thesedrugs from several companies, characterizing them, and noting any impurities or other unusual characteristics. We also developed a method to qualitatively assess the primancomponents prior to administration. Results: Most of the GS-441524 samples tested were similar in purity and composition, bothbetween batches and between brands. Most of the brands tested had concentrations of GS-41524 similar to the concentration advertised. 3 of the 17 types of vials tested hadconcentrations over 10% above advertised, and one was over 20% higher thanadvertised. One batch, known to have significant quality concems based on the lack ofefficacy in animals treated, had a concentration almost 50% below advertised. We alsctested 5 vials of GC376 and found 1/5 vials contained GS-441524 rather than GC376 and the other 4/5 vials contained Molnupiravir Conclusions: Most of the vials tested contained the advertised drug at the labeled concentration.Some of the GS-441524 vials were 10-25% more concentrated than advertised butgiven the low toxicity this is probably not of great concern. However, one batch hadapproximately half the expected concentration, which explains the reported lack ofefficacy. None of the GC376 vials tested contained GC376. GC376 is used in cats thatare unresponsive to GS-441524, and use of the wrong antiviral can cause serious sideeffects. in addition, we provide suggested methods for determining the purity of newbatches of these compounds and distinguishing one drug from the other.

Keywords: Feline coronavirus ; Feline infectious peritonitis ; GS-441524 ; GC376 ; Off-label Use ; Molnupiravir

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Product Details of GS-441524

CAS No. :1191237-69-0
Formula : C12H13N5O4
M.W : 291.26
SMILES Code : N#C[C@@]1(C2=CC=C3C(N)=NC=NN32)O[C@H](CO)[C@@H](O)[C@H]1O
MDL No. :MFCD32666994
InChI Key :BRDWIEOJOWJCLU-LTGWCKQJSA-N
Pubchem ID :44468216

Safety of GS-441524

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04859244 COVID-19 PHASE1 COMPLETED 2021-08-01 Copycat Sciences Study Site, H... More >>ouston, Texas, 77054, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.17mL

3.43mL

1.72mL

34.33mL

6.87mL

3.43mL

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