| Bioactivity | SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies[1]. |
| Invitro | SARS-CoV-2 Mpro-IN-2 (0.01-100 μM; 4 h) shows low cytotoxicity in Vero E6 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | SARS-CoV-2 Mpro-IN-2 (2 mg/kg; i.v.; single) exhibits clearance rate (CL), mean residence time (MRT), and half-life (t1/2) are 3140 mL/h/kg, 0.40 h, and 0.36 h, respectively[1].SARS-CoV-2 Mpro-IN-2 (10 mg/kg; p.o.; single) is rapidly absorbed, with a time-to-maximum concentration (Tmax) of 0.5 h, and shows a moderate pharmacokinetic profile including a favorable t1/2 (1.73 h), a maximum concentration (Cmax) 74.6 ng/mL, and an area under curve (AUC0-t) of 235 ng h/mL[1]. Animal Model: |
| Name | SARS-CoV-2 Mpro-IN-2 |
| CAS | 2768834-39-3 |
| Formula | C22H20Cl2N4O2S |
| Molar Mass | 475.39 |
| 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. Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity. J Med Chem. 2022 Sep 15:acs.jmedchem.2c01146. |