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.
- CAS No.: 3022242-53-8
- Formula: C25H25Cl3N4O4
- Molecular Weight:551.85
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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]
|
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] |
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.
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.
Chemical Information
-
CAS No. 3022242-53-8
-
Molecular Weight 551.85
-
Formula C25H25Cl3N4O4
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)