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SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CLpro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CLpro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19)[1]. | [in vivo]
SARS-CoV-2 3CLpro-IN-5 (oral, i.v.; 10, 100 mg/kg) has strong antiviral activity and favorable pharmacokinetic properties[1]. | Animal Model: | mice[1] | | Dosage: | 10, 100 mg/kg | | Administration: | oral (100 mg/kg) and intravenous (10 mg/kg) administration | | Result: | Showed the plasma concentration was 15.2 μM after 1 h and decreased to 0.40 μM over 6 h after oral administration (100 mg/kg) .
Showed the plasma concentration reached 9.3 μM after 1 h and decreased to 0.33 μM after 6 h in intravenous administration (10 mg/kg) .
Had approximately 9.0% estimated bioavailability (BA).
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| [References]
[1] Yuya Hirose, et al. Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. J Med Chem DOI:10.1021/acs.jmedchem.2c01081 |
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