GC376

Catalog No.S0475 Batch:S047503

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Technical Data

Formula

C21H30N3NaO8S

Molecular Weight 507.53 CAS No. 1416992-39-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (197.03 mM)
Ethanol 100 mg/mL (197.03 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GC376 is a 3CLpro (3C-like protease) inhibitor with IC50 of ~ 1.11 μM for the PEDV 3CLpro. GC376 is active against the 3CLpro of multiple coronaviruses, including SARS-CoV.
Targets
PEDV 3CLpro [1]
(Cell-free assay)
1.11 μM
In vitro

Molnupiravir and GC376 show a synergistic activity on SARS-CoV-2 at 48 h, and an additive activity on SARS-CoV-2 at 72 h.[2]

In vivo

GC376, a dipeptidyl bisulfite adduct salt, is a 3CLpro (3C-like protease) inhibitor that exerts strong inhibitory effects on picornaviruses and coronaviruses, including SARS-CoV.

Protocol (from reference)

Cell Assay:

[2]

  • Cell lines

    Vero E6 cells

  • Concentrations

    0.21-16.7 μM

  • Incubation Time

    48 and 72 h

  • Method

    Vero E6 cells (3000 cells/well) were seeded in 96-well clear flat-bottom plates and incubated at 37°C with 5% CO2 for 24 h. After incubation, cells were infected using a multiplicity of infection (MOI) of 0.1. SARS-CoV-2 was allowed to adsorb for one hour at 37°C. Subsequently, virus inoculum was removed, and cells were overlaid with media containing 3-fold serial dilutions of molnupiravir (0.62-50 μM), nirmatrelvir (0.62-50 μM) and GC376 (0.21-16.7 μM). Negative controls (compounds alone), infected positive controls (SARS-CoV-2 alone) and mock-infected cells were included in each plate. Plates were incubated at 37°C with 5% CO2 for 48 and 72 h and then, cell viability was measured using an MTT reduction assay.

    (Data sourced from selleck products)

Animal Study:

[3]

  • Animal Models

    Female BALB/c mice

  • Dosages

    111 or 55.5 mg/kg

  • Administration

    i.m.

Selleck's GC376 has been cited by 23 publications

Enterovirus D68 3C protease antagonizes type I interferon signaling by cleaving signal transducer and activator of transcription 1 [ J Virol, 2024, 98(2):e0199423] PubMed: 38240591
An RNA replicon system to investigate promising inhibitors of feline coronavirus [ J Virol, 2024, e0121623.] PubMed: 38236006
A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16] PubMed: 36803605
Insights into the mechanism of SARS-CoV-2 main protease autocatalytic maturation from model precursors [ Commun Biol, 2023, 10.1038/s42003-023-05469-8] PubMed: 37957287
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] PubMed: 37047038
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062] PubMed: None
Enterovirus D68 Infection Induces TDP-43 Cleavage, Aggregation, and Neurotoxicity [ J Virol, 2023, 97(4):e0042523] PubMed: 37039659
Lichen or Associated Micro-Organism Compounds Are Active against Human Coronaviruses [ Viruses, 2023, 15(9)1859] PubMed: 37766264
Construction and characterization of two SARS-CoV-2 minigenome replicon systems [ J Med Virol, 2022, 10.1002/jmv.27650] PubMed: 35137972
Modulation of the monomer-dimer equilibrium and catalytic activity of SARS-CoV-2 main protease by a transition-state analog inhibitor [ Commun Biol, 2022, 5(1):160] PubMed: 35233052

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.