GC376

Catalog No.S0475 Batch:S047503

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 1 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 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.

* <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.

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.

References

Selleck's GC376 has been cited by 30 publications

Development of a Biosafety Level 1 Cellular Assay for Identifying Small-Molecule Antivirals Targeting the Main Protease of SARS-CoV-2: Evaluation of Cellular Activity of GC376, Boceprevir, Carmofur, Ebselen, and Selenoneine [ Int J Mol Sci, 2024, 25(11)5767]	PubMed: 38891954
An efficient trans complementation system for in vivo replication of defective poliovirus mutants [ J Virol, 2024, 98(7):e0052324]	PubMed: 38837378
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
Design of novel and highly selective SARS-CoV-2 main protease inhibitors [ Antimicrob Agents Chemother, 2024, 68(10):e0056224]	PubMed: 39225484
Characterization of alternate encounter assemblies of SARS-CoV-2 main protease [ J Biol Chem, 2024, S0021-9258(24)02176-8]	PubMed: 39128719
SARS-CoV-2 Mpro inhibitor identification using a cellular gain-of-signal assay for high-throughput screening [ SLAS Discov, 2024, S2472-5552(24)00043-1]	PubMed: 39173830
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, 10.3390/ijms24076062]	PubMed: None

RETURN POLICY
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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.