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编 号：F762928
分子式：C34H43FN4O7
分子量：638.73
分子式：C34H43FN4O7
分子量：638.73
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CAS No: 3023276-79-8
产品详情
生物活性：
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (MPro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM.
体内研究：
SARS-CoV-2 Mpro-IN-5 (SM142) (10 mg/kg for i.n. or 25 mg/kg for i.p.) protects K18-ACE2 mice from SARS-CoV2-induced weight loss and lethality.SARS-CoV-2 Mpro-IN-5 (3 mg/kg, i.v.) shows a half-life of 2.1 h and high clearance of 18490 mL/min/kg in in male C57Bl/6 mice.SARS-CoV-2 Mpro-IN-5 (10 mg/kg, p.o.) shows oral bioavailability of 37.5%.Animal Model:K18-hACE2 transgenic mice
Dosage:10 mg/kg (i.n.) or 25 mg/kg (i.p.)
Administration:Intranasal inhalation (i.n.), once daily for 3 days, prior to the infection; or Intraperitoneal injection (i.p.), twice daily for 5 days, postinfection administration.
Result:Prevented weight loss and prolonged survival.
体外研究：
SARS-CoV-2 Mpro-IN-5 (SM142) blocks SARS-CoV2 replication in A549-hACE2 cells with IC50 value of 14.7 nM.SARS-CoV-2 Mpro-IN-5 (0-50 μM, 24 h) cause cytotoxicity in A549-hACE2 cells.SARS-CoV-2 Mpro-IN-5 inhibits OC-43 virus mRNA expression A549 cells.SARS-CoV-2 Mpro-IN-5 inhibits SARS-CoV2 infection by inhibiting both MPro and CatL.
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (MPro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM.
体内研究：
SARS-CoV-2 Mpro-IN-5 (SM142) (10 mg/kg for i.n. or 25 mg/kg for i.p.) protects K18-ACE2 mice from SARS-CoV2-induced weight loss and lethality.SARS-CoV-2 Mpro-IN-5 (3 mg/kg, i.v.) shows a half-life of 2.1 h and high clearance of 18490 mL/min/kg in in male C57Bl/6 mice.SARS-CoV-2 Mpro-IN-5 (10 mg/kg, p.o.) shows oral bioavailability of 37.5%.Animal Model:K18-hACE2 transgenic mice
Dosage:10 mg/kg (i.n.) or 25 mg/kg (i.p.)
Administration:Intranasal inhalation (i.n.), once daily for 3 days, prior to the infection; or Intraperitoneal injection (i.p.), twice daily for 5 days, postinfection administration.
Result:Prevented weight loss and prolonged survival.
体外研究：
SARS-CoV-2 Mpro-IN-5 (SM142) blocks SARS-CoV2 replication in A549-hACE2 cells with IC50 value of 14.7 nM.SARS-CoV-2 Mpro-IN-5 (0-50 μM, 24 h) cause cytotoxicity in A549-hACE2 cells.SARS-CoV-2 Mpro-IN-5 inhibits OC-43 virus mRNA expression A549 cells.SARS-CoV-2 Mpro-IN-5 inhibits SARS-CoV2 infection by inhibiting both MPro and CatL.
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