1. Cell Cycle/DNA Damage
    Anti-infection
  2. DNA/RNA Synthesis
    SARS-CoV
  3. GS-441524

GS-441524 

Cat. No.: HY-103586 Purity: 99.77%
Handling Instructions

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

GS-441524 Chemical Structure

CAS No. : 1191237-69-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 62 In-stock
Estimated Time of Arrival: December 31
5 mg USD 56 In-stock
Estimated Time of Arrival: December 31
10 mg USD 88 In-stock
Estimated Time of Arrival: December 31
50 mg USD 238 In-stock
Estimated Time of Arrival: December 31
100 mg USD 357 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target

EC50: 0.78 μM (FIPV)[1].

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].

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].

Molecular Weight

291.26

Formula

C₁₂H₁₃N₅O₄

CAS No.

1191237-69-0

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (429.17 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 4.

    Add each solvent one by one:  5% ethanol, 30% propylene glycol, 45% PEG 400, 20% water (pH 1.5 with HCI)

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

*All of the co-solvents are provided by MCE.
References
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
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Keywords:

GS-441524GS441524GS 441524DNA/RNA SynthesisSARS-CoVSARS coronavirusfelineinfectiousperitonitisvirusFIPVInhibitorinhibitorinhibit

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GS-441524
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HY-103586
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