1. Anti-infection
  2. SARS-CoV
  3. GC-78-HCl

GC-78-HCl is an orally and nonpeptidic SARS-CoV-2 Mpro inhibitor, with an IC50 of 0.19 μM for enzyme. GC-78-HCl has excellent antiviral activity and favorable pharmacokinetic properties.

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

GC-78-HCl

GC-78-HCl Chemical Structure

CAS No. : 3022242-53-8

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Description

GC-78-HCl is an orally and nonpeptidic SARS-CoV-2 Mpro inhibitor, with an IC50 of 0.19 μM for enzyme. GC-78-HCl has excellent antiviral activity and favorable pharmacokinetic properties[1].

IC50 & Target

EC50 Tatget: SARS-CoV[1] EC50: 0.40 μM (SARS-CoV-2), 0.21 ± 0.030 μM (wild-type), 0.21 ± 0.080 μM (Alpha), 0.24 ± 0.080 μM (Delta), 0.25 ± 0.060 μM (Omicron B.1)[1]

Cellular Effect
Cell Line Type Value Description References
Vero C1008 CC50
86 μM
Compound: GC-78-HCl
Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
[PMID: 37992202]
In Vitro

GC-78-HCl (0.01-10 μM) has low cytotoxicity in Vero E6 cells[1].
GC-78-HCl exhibits potent antiviral activity against SARS-CoV-2 variants and other human coronaviruses in MRC-5/Vero E6 cells, indicates its potential broad-spectrum anticoronaviral activity[1].
GC-78-HCl (50 μM) has no inhibitory activity against human cathepsins B/F/K/L and Caspase 3, indicates high target specificity toward coronavirus proteases[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GC-78-HCl (800 mg/kg, p.o., single dosage) has no acute toxicity in Kunming mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague−Dawley rats[1]
Dosage: 2 mg/kg
Administration: Intravenous injection (i.v.)
Result: With the clearance rate (CL) of 4343 mL/h/kg.
With half-life (t1/2) of 0.46 h.
Animal Model: Sprague−Dawley rats[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: With half-life (t1/2) of 1.64 h.
With time-to-maximum concentration (Tmax) of 1.17 h.
With maximum concentration (Cmax) of 148 ng/mL.
With an area under curve (AUC0‑t) of 465 ng•h/mL.
Animal Model: Kunming rats[1]
Dosage: 800 mg/kg
Administration: Oral gavage (p.o.)
Result: Exhibited no significant change in mice weight.
Molecular Weight

551.85

Formula

C25H25Cl3N4O4

CAS No.
SMILES

O=C([C@@H]1CN(CCN1C2=CC(Cl)=C(Cl)C=C2)C(C3=CN=CC=C3OC)=O)NC4=CC=C(C=C4)OC.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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GC-78-HCl Related Classifications

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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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Product Name:
GC-78-HCl
Cat. No.:
HY-149774
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