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编 号：F756798
分子式：C22H26ClF2N5O4
分子量：497.92
分子式：C22H26ClF2N5O4
分子量：497.92
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CAS No: 2913186-57-7
产品详情
生物活性：
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).
体内研究：
SARS-CoV-2 3CLpro-IN-5 (oral, i.v.; 10, 100 mg/kg) has strong antiviral activity and favorable pharmacokinetic properties.Animal Model:mice
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).
体外研究：
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 antiviral activity in 293TAT cells againsts various SARS-CoV-2 strains α, δ, Om BA.1 and Om BA.2 with EC50 values of 13.8 nM, 7.57 nM, 9.01 nM and 17.1 nM, respectively.SARS-CoV-2 3CLpro-IN-5 has antiviral activity against various coronaviruses SARS-CoV (293TAT cells), MERS-CoV (293TDPP4 cells) and HCoV-OC43 (293TAT cells) with EC50 values of 59.3 nM, 4.72 nM and 1.67 nM, respectively.
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).
体内研究：
SARS-CoV-2 3CLpro-IN-5 (oral, i.v.; 10, 100 mg/kg) has strong antiviral activity and favorable pharmacokinetic properties.Animal Model:mice
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).
体外研究：
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 antiviral activity in 293TAT cells againsts various SARS-CoV-2 strains α, δ, Om BA.1 and Om BA.2 with EC50 values of 13.8 nM, 7.57 nM, 9.01 nM and 17.1 nM, respectively.SARS-CoV-2 3CLpro-IN-5 has antiviral activity against various coronaviruses SARS-CoV (293TAT cells), MERS-CoV (293TDPP4 cells) and HCoV-OC43 (293TAT cells) with EC50 values of 59.3 nM, 4.72 nM and 1.67 nM, respectively.
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