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 Chemical Structure

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]

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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