Art. -Nr.: HY-103586

GS-441524

27 Cited Publications

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GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19).

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Reinheit: 99.89%
CAS. Nr.: 1191237-69-0
Formel: C₁₂H₁₃N₅O₄
Molecular Weight:291.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GS-441524 Chemical Structure

CAS. Nr.: 1191237-69-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- Clinical Trial
Chemical Information
Publications (27)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 0.78 μM (FIPV)^[1].

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-3	CC₅₀	>100 μM Compound: RVnb; GS-441524	Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability incubated for 48.5 hrs by CellTiter-Glo assay Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability incubated for 48.5 hrs by CellTiter-Glo assay	[PMID: 37040439]
Fibroblast	CC₅₀	>100 μM Compound: GS-441524	Cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay Cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay	[PMID: 33877845]
HEL 299	CC₅₀	>100 μM Compound: GS-441524	Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay	[PMID: 35571875]
HeLa	CC₅₀	>20 μM Compound: Page no 2220, R7C1	Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
HeLa	CC₅₀	>30 μM Compound: 3a	Cytotoxicity against human HeLa cells by MTS assay Cytotoxicity against human HeLa cells by MTS assay	[PMID: 22446091]
HeLa	EC₅₀	>20 μM Compound: 4	Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay	[PMID: 28124907]
HeLa	EC₅₀	>20 μM Compound: Page no 2220, R7C1	Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay	[PMID: 28792763]
HeLa	EC₅₀	11 μM Compound: 3a	Antiviral activity against Yellow fever virus 17D infected in human HeLa cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Yellow fever virus 17D infected in human HeLa cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
HEp-2	CC₅₀	>100 μM Compound: 4	Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay	[PMID: 28124907]
HEp-2	CC₅₀	>100 μM Compound: 4	Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay	[PMID: 33835812]
HEp-2	EC₅₀	0.53 μM Compound: 4	Antiviral activity against RSV A2 infected in HEp-2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by CellTiter Glo viability assay Antiviral activity against RSV A2 infected in HEp-2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by CellTiter Glo viability assay	[PMID: 33835812]
HEp-2	IC₅₀	0.35 μM Compound: 4	Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis	[PMID: 33835812]
Hepatocyte	CC₅₀	>100 μM Compound: 2; GS-441524	Cytotoxicity against human primary hepatocytes assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human primary hepatocytes assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
HepG2	CC₅₀	>100 μM Compound: 2; GS-441524	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
Huh-7	CC₅₀	>20 μM Compound: Page no 2220, R7C1	Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
Huh-7	CC₅₀	>88 μM Compound: 4	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay	[PMID: 28124907]
Huh-7	CC₅₀	>89 μM Compound: 3a	Cytotoxicity against human HuH7 cells by MTS assay Cytotoxicity against human HuH7 cells by MTS assay	[PMID: 22446091]
Huh-7	CC₅₀	>89 μM Compound: 4	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 3 days by dual-Glo luciferase assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 3 days by dual-Glo luciferase assay	[PMID: 33835812]
Huh-7	CC₅₀	>89 μM Compound: 2; GS-441524	Cytotoxicity against human Huh-7 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
Huh-7	EC₅₀	4.1 μM Compound: 3a	Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
Macrophage	CC₅₀	>20 μM Compound: Page no 2220, R7C1	Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
Macrophage	CC₅₀	>64 μM Compound: 7; GS-441524	Cytotoxicity against mouse primary macrophages assessed as reduction in cell viability Cytotoxicity against mouse primary macrophages assessed as reduction in cell viability	[PMID: 33385837]
MDCK	CC₅₀	>30 μM Compound: 3a	Cytotoxicity against dog MDCK cells by MTS assay Cytotoxicity against dog MDCK cells by MTS assay	[PMID: 22446091]
MDCK	EC₅₀	27.9 μM Compound: 3a	Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
MRC5	CC₅₀	>30 μM Compound: 3a	Cytotoxicity against human MRC5 cells by MTS assay Cytotoxicity against human MRC5 cells by MTS assay	[PMID: 22446091]
MRC5	CC₅₀	>89 μM Compound: 2; GS-441524	Cytotoxicity against human MRC5 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human MRC5 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
MRC5	EC₅₀	>30 μM Compound: 3a	Antiviral activity against Coxsackievirus A21 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Coxsackievirus A21 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
MRC5	EC₅₀	>30 μM Compound: 3a	Antiviral activity against Coxsackievirus A7 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Coxsackievirus A7 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
MT4	CC₅₀	>50 μM Compound: 4	Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by CellTiter Glo viability assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by CellTiter Glo viability assay	[PMID: 33835812]
MT4	CC₅₀	>500 μM Compound: GS-441524	Cytotoxicity against human MT4 cells assessed as reduction in cell viability treated for 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability treated for 5 days by MTT assay	[PMID: 37229831]
MT4	CC₅₀	>57 μM Compound: 4	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay	[PMID: 28124907]
MT4	CC₅₀	69 μM Compound: 2; GS-441524	Cytotoxicity against human MT4 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
PBMC	CC₅₀	>100 μM Compound: 2; GS-441524	Cytotoxicity against quiescent human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against quiescent human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
PBMC	CC₅₀	>100 μM Compound: 2; GS-441524	Cytotoxicity against stimulated human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against stimulated human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
PC-3	CC₅₀	>100 μM Compound: 2; GS-441524	Cytotoxicity against human PC-3 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay Cytotoxicity against human PC-3 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 37596939]
Vero	CC₅₀	>30 μM Compound: 3a	Cytotoxicity against african green monkey Vero cells by MTS assay Cytotoxicity against african green monkey Vero cells by MTS assay	[PMID: 22446091]
Vero	CC₅₀	>30 μM Compound: 3a	Cytotoxicity against african green monkey Vero E6 cells by MTS assay Cytotoxicity against african green monkey Vero E6 cells by MTS assay	[PMID: 22446091]
Vero	EC₅₀	>30 μM Compound: 3a	Antiviral activity against West nile virus NY99 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against West nile virus NY99 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
Vero	EC₅₀	1.71 μM Compound: 3a	Antiviral activity against Parainfluenza 3 C 243 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Parainfluenza 3 C 243 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
Vero	EC₅₀	2.24 μM Compound: 3a	Antiviral activity against SARS coronavirus Toronto-2 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against SARS coronavirus Toronto-2 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
Vero	EC₅₀	9.46 μM Compound: 3a	Antiviral activity against Dengue virus type 2 New Guinea C infected in african green monkey Vero E6 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay Antiviral activity against Dengue virus type 2 New Guinea C infected in african green monkey Vero E6 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay	[PMID: 22446091]
Vero C1008	CC₅₀	72.38 μM Compound: GS-441524	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 1 to 2 hrs by MTS assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 1 to 2 hrs by MTS assay	[PMID: 33962311]
Vero C1008	CC₅₀	72.9 μM Compound: GS-441524	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay	[PMID: 35571875]
Vero C1008	EC₅₀	0.39 μM Compound: GS-441524	Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in infection measured after 24 hrs by Plaque assay Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in infection measured after 24 hrs by Plaque assay	[PMID: 37229831]

In Vitro

GS-441524 (1.2-100 μM; 24-72 h) shows no cytotoxicity to Crandell-Rees feline kidney (CRFK) cells, with a CC₅₀ >100 μM^[1].
GS-441524 (0-3 μM; 72 h) dose-dependently inhibits FIPV-79-1146-induced CPE in CRFK cells, with an EC₅₀ of 0.78 μM^[1].
GS-441524 (0.1-50 μM; 20 h) inhibits FIPV-79-1146 RNA replication in CRFK cells^[1].
GS-441524 (10 μM; 20-72 h) potently inhibits wild-type FIPV RNA replication in naturally infected feline peritoneal macrophages^[1].
GS-441524 (1 μM; 6-72 h) is internalized by CRFK cells, phosphorylated to its active triphosphate form^[1].
GS-441524 (20-800 μM; 72 h) exhibits cytotoxicity toward porcine alveolar macrophages with a CC₅₀ of 287.51 μM, with minimal cytotoxicity at concentrations ≤200 μM^[2].
GS-441524 (20-200 μM; 48 h) inhibits African swine fever virus replication in porcine alveolar macrophages in vitro in a dose-dependent manner, with an EC₅₀ of 73.2 μM, reducing viral titer, mRNA levels, and protein expression^[2].
GS-441524 (100 μM; 0-16 h post-infection) inhibits African swine fever virus replication in porcine alveolar macrophages^[2].
GS-441524 (100 μM; 48 h) shows an inhibitory effect on African swine fever virus replication in porcine alveolar macrophages, which is dose-dependently attenuated by ATP, while does not alter the levels of IFN-α, IFN-β, TNF-α, or IL-6^[2].
GS-441524 potently inhibits SARS-CoV-2 in multiple cell lines, with a median IC₅₀ of 0.87 μM and median IC₉₀ of 1.42 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[1]

Cell Line:

FIPV-79-1146-infected CRFK cells
Concentration:

0, 0.1, 1.0, 10, 50 μM
Incubation Time:

20 h
Result:

Achieved complete inhibition of viral RNA expression at 50 and 10 μM.
Achieved partial inhibition of viral RNA expression at 1.0 μM.
Caused no inhibition of viral RNA expression at 0.1 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:

Crandell-Rees feline kidney (CRFK) cells
Concentration:

1.2, 3.7, 11.1, 33.3, 100 μM (24 h); 10 μM (72 h)
Incubation Time:

24; 72 h
Result:

Showed no uptake of CellTox Green dye at all tested concentrations.
Caused no cytopathic effect observed visually or via crystal violet staining quantitation at all tested concentrations.
Exhibited the cytotoxic concentration-50% (CC_{50_{) to be >100 μM.}}

Real Time qPCR^[1]

Cell Line:

Naturally FIPV-infected feline peritoneal macrophages
Concentration:

10 μM
Incubation Time:

20; 72 h
Result:

Reduced cell-associated FIPV RNA transcripts by approximately 1000-fold relative to untreated cells at 10 μM for 20 h.
Caused a significant reduction in cell-associated FIPV RNA relative to untreated cells at 10 μM for 72 h.

Cell Cytotoxicity Assay^[2]

Cell Line:

porcine alveolar macrophages (PAMs)
Concentration:

20, 50, 100, 200, 400, 800 μM
Incubation Time:

72 h
Result:

Reduced PAM survival rate to 30% at 400 μM.
Maintained cell survival rate over 85% at concentrations ≤200 μM with no obvious morphological difference from untreated cells.
Exhibited a CC₅₀ of 287.51 μM.

Real Time qPCR^[2]

Cell Line:

porcine alveolar macrophages (PAMs) infected with African swine fever virus (ASFV) strain GZ201801
Concentration:

100 μM
Incubation Time:

0, 1, 3, 6, 9, 12, 16 h post-infection
Result:

Significantly inhibited transcription of the early ASFV gene CP204L starting at 1 h post-infection, with increasingly significant effects over time.
Inhibited transcription of the late ASFV gene B646L first observed at 6 h post-infection.

Real Time qPCR^[2]

Cell Line:

porcine alveolar macrophages (PAMs) with or without African swine fever virus (ASFV) strain GZ201801 infection
Concentration:

100 μM
Incubation Time:

48 h
Result:

Showed no significant differences in IFN-α, IFN-β, TNF-α, or IL-6 levels.
Showed significant differences in ATP concentrations in different treatment groups.

Parmacokinetics

Species	Dose	Route	AUC_0-inf
Cat^[3]	5 mg/kg	i.v.	42.42 μM·h
Cat^[3]	5 mg/kg	s.c.	41.26 μM·h
Mice^[3]	10 mg/kg	p.o.	8.71 μM·h
Mice^[3]	5 mg/kg	i.v.	11.08 μM·h
Rat^[3]	10 mg/kg	p.o.	7.47 μM·h
Rat^[3]	30 mg/kg	i.g.	68.64 μM·h
Rat^[3]	30 mg/kg	i.v.	1875.28 μM·h

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1191237-69-0
Appearance Solid
Molecular Weight 291.26
Formel C₁₂H₁₃N₅O₄
Color White to off-white
SMILES

N#C[C@@]1(C2=CC=C3N2N=CN=C3N)O[C@H](CO)[C@@H](O)[C@H]1O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (27)

All Cell Proliferation/Viability AssayMicrobiological AssayPK/PD Analysis

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Journal Impact Factor

Nature

A coronavirus assembly inhibitor that targets the viral membrane protein. [Abstract]

2025 Apr;640(8058):514-523. PMID: 40140569
Nat Commun

Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets. [Abstract]

2021 Nov 5;12(1):6415. PMID: 34741049

GS-441524 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Nov 5;12(1):6415. [Abstract]

Virus yield reduction of SARS-CoV-2 clinical isolates WA1/2020 (red squares), CA/2020 (blue triangles), SA/2020 (green diamonds), and BZ/2021 (yellow triangles) representing the A, B.1.1.7 (α), B.1.351 (β) and P.1 (γ) lineages, respectively, by GS-441524 (0.1-10 μM; 48 h) on VeroE6 cells.

GS-441524 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Nov 5;12(1):6415. [Abstract]

In vitro cytotoxicity profiles of GS-441524 (0.01-100 μM; 72 h) on VeroE6 (blue squares), HEp-2 (purple circles), BHK-21 (light blue triangles), HCT-8 (green triangles) and a panel of primary HAE cells from independent donors (“F2” (yellow diamonds), “F3” (orange circles), “M2” (red “×” symbols), “M6” (brown “+” symbols), “DF2” (black stars)).

GS-441524 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Nov 5;12(1):6415. [Abstract]

Single dose pharmacokinetic parameters of GS-441524 (20 mg/kg)following administration of either intravenous GS-441524 or remdesivir or oral GS-621763 in ferrets
^aapproximately 10 nM GS-621763 transiently observed in first two hours

GS-441524 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Nov 5;12(1):6415. [Abstract]

Single-dose PK study in ferrets showing plasma concentrations of GS-441524, GS-621763, and remdesivir (RDV) as specified after dosing with GS-621763 (30 mg/kg; p.o.; red “+” symbols), remdesivir (10 mg/kg; i.v.; blue “×” symbols), and GS-441524 (20 mg/kg; i.v.; green triangles). Symbols represent individual biological repeats (n = 3), lines depict sample means.
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Nano Lett

Nanopore Signatures of Nucleoside Drugs. [Abstract]

2023 Oct 25;23(20):9437-9444. PMID: 37818841
Biomed Pharmacother

Remdesivir inhibits the progression of glioblastoma by enhancing endoplasmic reticulum stress. [Abstract]

2023 Jan:157:114037. PMID: 36427388
J Med Chem

Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung. [Abstract]

2024 May 9;67(9):7470-7486. PMID: 38690769
Vet Q

Antiviral activity of Vigna radiata extract against feline coronavirus in vitro. [Abstract]

2024 Dec;44(1):1-13. PMID: 38712855
Int J Mol Sci

Baicalin Inhibits FIPV Infection In Vitro by Modulating the PI3K-AKT Pathway and Apoptosis Pathway. [Abstract]

2024 Sep 14;25(18):9930. PMID: 39337417
J Med Virol

In vitro activity of itraconazole against SARS-CoV-2. [Abstract]

2021 Jul;93(7):4454-4460. PMID: 33666253
ACS Omega

Efficacious Preclinical Repurposing of the Nucleoside Analogue Didanosine against COVID-19 Polymerase and Exonuclease. [Abstract]

2022 Jun 13;7(25):21385-21396. PMID: 35785294
ACS Omega

Potent Inhibitory Activities of the Adenosine Analogue Cordycepin on SARS-CoV-2 Replication. [Abstract]

2022 Jan 11;7(3):2960-2969. PMID: 35071937
FEBS J

Derivatives of MOPS: promising scaffolds for SARS coronaviruses Macro domain-targeted inhibition. [Abstract]

2025 Jun;292(11):2865-2881. PMID: 40070175
iScience

Antiviral efficacy against and replicative fitness of an XBB.1.9.1 clinical isolate. [Abstract]

2023 Oct 4;26(11):108147. PMID: 37876803
ACS Chem Biol

A Fluorescence Polarization Assay for Macrodomains Facilitates the Identification of Potent Inhibitors of the SARS-CoV-2 Macrodomain. [Abstract]

2023 May 19;18(5):1200-1207. PMID: 37126856
Vet Res

Development and characterization of reverse genetics systems of feline infectious peritonitis virus for antiviral research. [Abstract]

2024 Sep 27;55(1):124. PMID: 39334482
Clin Transl Sci

Exploration for the effect of renal function and renal replacement therapy on pharmacokinetics of remdesivir and GS-441524 in patients with COVID-19: A limited case series. [Abstract]

2022 Mar;15(3):732-740. PMID: 34761554
Virology

Cepharanthine: A promising natural compound against feline infectious peritonitis virus infection and associated inflammation. [Abstract]

2025 Jan 23:604:110422. PMID: 39884162
Vet Sci

Comparative Evaluation of GS-441524, Teriflunomide, Ruxolitinib, Molnupiravir, Ritonavir, and Nirmatrelvir for In Vitro Antiviral Activity against Feline Infectious Peritonitis Virus. [Abstract]

2023 Aug 9;10(8):513. PMID: 37624300

GS-441524 purchased from MedChemExpress. Usage Cited in: Vet Sci. 2023 Aug 9;10(8):513. [Abstract]

The CC₅₀, EC₅₀, and SI for six compounds against FIPV. The half-maximal cytotoxic concentration (CC₅₀) values are from four measurements of diluted drugs using MTT assay, in CRFK cells treated with drugs for 48 h. The half-maximal effective concentration (EC₅₀) values are from six measurements of diluted drugs against FIPV replication in CRFK cells for 48 h. Based on the SI value (mean CC₅₀)/(mean EC₅₀), GS-441524 was found highly selective (SI 165.5) against FIPV among the drugs tested and showed high efficacy (EC₅₀ 1.6 µM) against FIPV with a less deleterious effect (CC₅₀ 260.0 µM) on the cells. Nirmatrelvir also showed promising efficacy (EC₅₀ 2.5 µM) and selectivity (SI 113.7) against FIPV. Ritonavir showed the highest toxicity level in the cells (CC₅₀ 39.9).
J Feline Med Surg

Investigation of monotherapy and combined anticoronaviral therapies against feline coronavirus serotype II in vitro. [Abstract]

2022 Oct;24(10):943-953. PMID: 34676775
J Am Vet Med Assoc

Unlicensed antiviral products used for the at-home treatment of feline infectious peritonitis contain GS-441524 at significantly different amounts than advertised. [Abstract]

2024 Feb 7;262(4):489-497. PMID: 38324994
Biomed Res

Possible involvement of neuropeptide Y sub-receptor 1 (NPY-Y1) in the anti-viral response of SARS-CoV-2 infection in Syrian hamster. [Abstract]

2025;46(2):37-50. PMID: 40189329
bioRxiv

2026 Jun 10.
SSRN

2023 Sep 11.
Utah State University

2023 Feb 1.
bioRxiv

Broad-spectrum in vitro antiviral activity of ODBG-P-RVn: an orally-available, lipid-modified monophosphate prodrug of remdesivir parent nucleoside (GS-441524). [Abstract]

2021 Aug 10:2021.08.06.455494. PMID: 34401879
Research Square Preprint

2021 Aug.
bioRxiv

2020 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 83.33 mg/mL (286.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4334 mL

17.1668 mL

34.3336 mL

5 mM

0.6867 mL

3.4334 mL

6.8667 mL

10 mM

0.3433 mL

1.7167 mL

3.4334 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% Ethanol 30% Propylene glycol 45% PEG400 20% Water (pH 1.5 with HCl)

Solubility: 10 mg/mL (34.33 mM); Clear solution; Need ultrasonic and adjust pH to 2 with HCl

Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.75 mg/mL (9.44 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (781 KB)
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- Portuguese - PT (781 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233. [Content Brief]

[2]. Huang Z, et al. GS-441524 inhibits African swine fever virus infection in vitro. Antiviral Res. 2021;191:105081. [Content Brief]

[3]. Rasmussen HB, et al. Nucleoside analog GS-441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid-19. Pharmacol Res Perspect. 2022;10(2):e00945. [Content Brief]

[4]. Pedersen NC, et al. Efficacy and safety of the nucleoside analog GS-441524 for treatment of cats with naturally occurring feline infectious peritonitis. J Feline Med Surg. 2019;21(4):271-281. [Content Brief]

[5]. Coggins SJ, et al. Outcomes of treatment of cats with feline infectious peritonitis using parenterally administered remdesivir, with or without transition to orally administered GS-441524. J Vet Intern Med. 2023;37(5):1772-1783. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4334 mL	17.1668 mL	34.3336 mL	85.8340 mL
	5 mM	0.6867 mL	3.4334 mL	6.8667 mL	17.1668 mL
	10 mM	0.3433 mL	1.7167 mL	3.4334 mL	8.5834 mL
	15 mM	0.2289 mL	1.1445 mL	2.2889 mL	5.7223 mL
	20 mM	0.1717 mL	0.8583 mL	1.7167 mL	4.2917 mL
	25 mM	0.1373 mL	0.6867 mL	1.3733 mL	3.4334 mL
	30 mM	0.1144 mL	0.5722 mL	1.1445 mL	2.8611 mL
	40 mM	0.0858 mL	0.4292 mL	0.8583 mL	2.1458 mL
	50 mM	0.0687 mL	0.3433 mL	0.6867 mL	1.7167 mL
	60 mM	0.0572 mL	0.2861 mL	0.5722 mL	1.4306 mL
	80 mM	0.0429 mL	0.2146 mL	0.4292 mL	1.0729 mL
	100 mM	0.0343 mL	0.1717 mL	0.3433 mL	0.8583 mL

Keywords

GS-441524

27 Cited Publications

100 mg Angebot einholen

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GS-441524

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Clinical Compound Library

Antiviral Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GS-441524

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (27)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GS-441524

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Clinical Compound Library

Antiviral Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GS-441524

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (27)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GS-441524 Related Classifications

HY-103586 Related Classifications