| Bioactivity | 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]. |
| Target | EC50 Tatget: SARS-CoV 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) |
| Invitro | GC-78-HCl (0.01-10 μM) 在 Vero E6 细胞中具有低细胞毒性[1]。GC-78-HCl 在 MRC-5 和 Vero E6 细胞中对 SARS-CoV-2 变体及人类其他冠状病毒表现出有效的抗病毒活性，表明其具有潜在的广谱抗冠状病毒活性[1]。GC-78-HCl (50 μM) 对人组织蛋白酶 B、F、K、L 和 Caspase 3 无抑制活性，表明对冠状病毒蛋白酶具有很高的靶向特异性[1]。 0 --> GC-78-HCl 相关抗体: |
| In Vivo | GC-78-HCl (800 mg/kg, 口服, 单独给药) 对Kunming 小鼠无急性毒性[1]。 Animal Model: |
| Name | GC-78-HCl |
| Formula | C25H25Cl3N4O4 |
| Molar Mass | 551.85 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gao S, et al. Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability. J Med Chem. 2023 Nov 22. |