GS-441524

Name: GS-441524
Brand: MedChemExpress
SKU: HY-103586
Rating: 5.0 (23 reviews)

Cat. No.: HY-103586 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC₅₀ of 0.78 μM.

For research use only. We do not sell to patients.

GS-441524 Chemical Structure

CAS No. : 1191237-69-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 28	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 28	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 20	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 25	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of GS-441524:

Remdesivir In-stock
GS-443902 Get quote
GS-441524 hydrochloride Get quote

23 Publications Citing Use of MCE GS-441524

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Biological Activity
Protocol
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References
Customer Review

Description

IC₅₀ & Target

EC50: 0.78 μM (FIPV)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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	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	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	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	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]
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	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]
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	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]
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	CC₅₀	> 30 μM Compound: 3a	Cytotoxicity against human MRC5 cells by MTS assay Cytotoxicity against human MRC5 cells 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	> 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]
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	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	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]

In Vitro

The cells appear and grow normally at all concentrations of GS-441524 and fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC₅₀) of GS-441524 is calculated to be 0.78 μM^[1].

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

In Vivo

All 10 treated cats have a rapid response to treatment and lymphocyte levels and rectal temperatures return to pre-infection levels and levels of the two asymptomatic cats. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized and transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others and reactions are inconsistent from one injection to the next and decreas over time^[1].
Remdesivi (IV injection) in NHP results in GS-441524 being present in serum at concentrations 1000-fold higher than Remdesivir throughout a 7-day treatment course^[3].

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

Clinical Trial

Molecular Weight

291.26

Formula

C₁₂H₁₃N₅O₄

CAS No.

1191237-69-0

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (251 KB) HNMR (260 KB) RP-HPLC (109 KB)

Handling Instructions (2659 KB)

References

[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]. Katherine Yang, et al. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815. [Content Brief]

[3]. Victoria C. Yan, et al. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020.

Cell Assay	To determine the toxicity of GS-441524 to CRFK cells n, CRFK cells are treated with 100, 33.3, 11.1, 3.7 or 1.2 μM GS-441524 for 24 h^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Cats^[1] The 10 cats that developed disease signs are divided into two groups and treated with either 5 mg/kg (Group A; n=5) or 2 mg/kg (Group B; n=5) GS-441524 SC q24 h starting three days after unequivocal clinical evidence of FIP (days 12-19 post infection). The two cats that do not develop disease signs serve as controls for normal blood lymphocyte counts and rectal temperature^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]. Katherine Yang, et al. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815. [Content Brief] [3]. Victoria C. Yan, et al. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020.

Complete Stock Solution Preparation Table

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

GS-441524 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GS-4415241191237-69-0GS441524GS 441524DNA/RNA SynthesisSARS-CoVSARS coronavirusfelineinfectiousperitonitisvirusFIPVInhibitorinhibitorinhibit

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GS-441524

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Other Forms of GS-441524:

GS-441524 Related Antibodies

23 Publications Citing Use of MCE GS-441524

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GS-441524 Related Antibodies

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Complete Stock Solution Preparation Table

GS-441524 Related Classifications

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