产品
编 号：F521999
分子式：C38H47N5O7S2
分子量：749.94
分子式：C38H47N5O7S2
分子量：749.94
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价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 923604-59-5
产品详情
生物活性：
Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
体内研究：
Simeprevir (TMC435) has moderate terminal elimination half-life (t1/2=1.5 h and 4.1 h for rat (3 mg/kg, p.o.), monkey (3 mg/kg, p.o.)).Simeprevir (TMC435350) exhibits a medium-slow rate of absorption, well distribution with the high concentration observed in the liver, and a low clearance.Pharmacokinetic Parameters of Simeprevir (TMC435350) in male Sprague-Dawley rats.IV (2 mg/kg) PO (10 mg/kg)
CL (L/h/kg)0.505
Vdss (h)0.49
AUC0-24 (μM·h)5.212.79
Cmax (μM)0.73
Tmax (h)3.0
T1/2 (h)2.8
F (%)11
Liver/plasma ratio at 6 h63.532
Animal Model:Sprague-Dawley (SD) rats and cynomolgus monkeys
Dosage:3 mg/kg
Administration:Oral administration
Result:Time at which peak concentration (Tmax) of 1 hour and 2 hour for rat and monkey, respectively.Concentration at 24 h after dosing (C24 h) of 0.9 and 2.3 ng/mL for rat and monkey, respectively.AUC0-24h=1173 and1409 ng ? h/mL for rat and monkey, respectively.
体外研究：
Simeprevir (TMC435) inhibits HCV in a dose-dependent manner in Huh7-Luc cells, with EC50 and EC90 values of 8 nM and 24 nM, respectively.Simeprevir (TMC435) inhibits NS3/4A proteases from HCV genotypes 1 to 6 with IC50s of 1/0.9/7/30/1.5/2.2/1.6 nM for 1a/1b/2b/3a/4/5/6, respectively.Simeprevir inhibits SARS-CoV-2 in Vero E6 cells with IC50s of 9.6±2.3 μM and 5.5±0.2 μM for Mpro and RdRp, respectively.
Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
体内研究：
Simeprevir (TMC435) has moderate terminal elimination half-life (t1/2=1.5 h and 4.1 h for rat (3 mg/kg, p.o.), monkey (3 mg/kg, p.o.)).Simeprevir (TMC435350) exhibits a medium-slow rate of absorption, well distribution with the high concentration observed in the liver, and a low clearance.Pharmacokinetic Parameters of Simeprevir (TMC435350) in male Sprague-Dawley rats.IV (2 mg/kg) PO (10 mg/kg)
CL (L/h/kg)0.505
Vdss (h)0.49
AUC0-24 (μM·h)5.212.79
Cmax (μM)0.73
Tmax (h)3.0
T1/2 (h)2.8
F (%)11
Liver/plasma ratio at 6 h63.532
Animal Model:Sprague-Dawley (SD) rats and cynomolgus monkeys
Dosage:3 mg/kg
Administration:Oral administration
Result:Time at which peak concentration (Tmax) of 1 hour and 2 hour for rat and monkey, respectively.Concentration at 24 h after dosing (C24 h) of 0.9 and 2.3 ng/mL for rat and monkey, respectively.AUC0-24h=1173 and1409 ng ? h/mL for rat and monkey, respectively.
体外研究：
Simeprevir (TMC435) inhibits HCV in a dose-dependent manner in Huh7-Luc cells, with EC50 and EC90 values of 8 nM and 24 nM, respectively.Simeprevir (TMC435) inhibits NS3/4A proteases from HCV genotypes 1 to 6 with IC50s of 1/0.9/7/30/1.5/2.2/1.6 nM for 1a/1b/2b/3a/4/5/6, respectively.Simeprevir inhibits SARS-CoV-2 in Vero E6 cells with IC50s of 9.6±2.3 μM and 5.5±0.2 μM for Mpro and RdRp, respectively.
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