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

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).

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

CAS No. : 1191237-69-0

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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of GS-441524:

Top Publications Citing Use of Products

    GS-441524 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 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.

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    • Biological Activity

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    • Customer Review

    Description

    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)[1][2][3][4][5].

    IC50 & Target

    EC50: 0.78 μM (FIPV)[1].

    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]
    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]
    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
    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]
    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]
    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]
    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]
    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: 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 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]
    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
    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]
    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]
    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]
    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 E6 cells by MTS assay
    Cytotoxicity against african green monkey Vero E6 cells 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 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 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 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% (CC50) 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 AUC0-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
    Molecular Weight

    291.26

    Formula

    C12H13N5O4

    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

    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
    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)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    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

    Purity: 99.92%

    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, 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
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    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.

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