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

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

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

CAS No. : 2378280-82-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of GS-441524 hydrochloride:

GS-441524 hydrochloride Related Antibodies

Top Publications Citing Use of Products

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

    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).

    GS-441524 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GS-441524 hydrochloride is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 hydrochloride competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 hydrochloride inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 hydrochloride reduces viral RNA levels in cats. GS-441524 hydrochloride can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19)[1][2][3][4][5].

    IC50 & Target[1]

    RNA Polymerase

     

    In Vitro

    GS-441524 (1.2-100 μM; 24-72 h) hydrochloride shows no cytotoxicity to Crandell-Rees feline kidney (CRFK) cells, with a CC50 >100 μM[1].
    GS-441524 (0-3 μM; 72 h) hydrochloride 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) hydrochloride inhibits FIPV-79-1146 RNA replication in CRFK cells[1].
    GS-441524 (10 μM; 20-72 h) hydrochloride potently inhibits wild-type FIPV RNA replication in naturally infected feline peritoneal macrophages[1].
    GS-441524 (1 μM; 6-72 h) hydrochloride is internalized by CRFK cells, phosphorylated to its active triphosphate form[1].
    GS-441524 (20-800 μM; 72 h) hydrochloride 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) hydrochloride 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) hydrochloride inhibits African swine fever virus replication in porcine alveolar macrophages[2].
    GS-441524 (100 μM; 48 h) hydrochloride 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 hydrochloride 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.

    GS-441524 hydrochloride Related Antibodies

    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% (CC50) to be >100 μM.

    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.

    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.

    RT-PCR[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 AUC0-inf
    Mice[3] 5 mg/kg i.v. 11.08 μM·h
    Mice[3] 10 mg/kg p.o. 8.71 μM·h
    Cat[3] 5 mg/kg s.c. 41.26 μM·h
    Cat[3] 5 mg/kg i.v. 42.42 μM·h
    Rat[3] 30 mg/kg i.v. 1875.28 μM·h
    Rat[3] 30 mg/kg i.g. 68.64 μM·h
    Rat[3] 10 mg/kg p.o. 7.47 μM·h
    Molecular Weight

    327.72

    Formula

    C12H14ClN5O4
    CAS No.
    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.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (305.14 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 3.0514 mL 15.2569 mL 30.5139 mL
    5 mM 0.6103 mL 3.0514 mL 6.1028 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    • Dilution Calculator

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

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    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (15.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 2

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

      Solubility: ≥ 5 mg/mL (15.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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
    References

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0514 mL 15.2569 mL 30.5139 mL 76.2846 mL
    5 mM 0.6103 mL 3.0514 mL 6.1028 mL 15.2569 mL
    10 mM 0.3051 mL 1.5257 mL 3.0514 mL 7.6285 mL
    15 mM 0.2034 mL 1.0171 mL 2.0343 mL 5.0856 mL
    20 mM 0.1526 mL 0.7628 mL 1.5257 mL 3.8142 mL
    25 mM 0.1221 mL 0.6103 mL 1.2206 mL 3.0514 mL
    30 mM 0.1017 mL 0.5086 mL 1.0171 mL 2.5428 mL
    40 mM 0.0763 mL 0.3814 mL 0.7628 mL 1.9071 mL
    50 mM 0.0610 mL 0.3051 mL 0.6103 mL 1.5257 mL
    60 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2714 mL
    80 mM 0.0381 mL 0.1907 mL 0.3814 mL 0.9536 mL
    100 mM 0.0305 mL 0.1526 mL 0.3051 mL 0.7628 mL
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    GS-441524 hydrochloride Related Classifications

    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-4415242378280-82-9GS441524GS 441524DNA/RNA SynthesisSARS-CoVSARS coronavirusfeline infectious peritonitisCRFK cellsporcine alveolar macrophagesCOVID-19feline peritoneal macrophagescatsfeline infectious peritonitis virussevere acute respiratory syndrome coronavirus 2African swine fever virusviral RNA-dependent RNA polymeraseInhibitorinhibitorinhibit

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