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Simeprevir sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Simeprevir sodium图片
CAS NO:1241946-89-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
西咪匹韦钠
TMC435 sodium
TMC435350 sodium
产品介绍
Simeprevir (TMC435; TMC435350) sodium 是一种有效、高特异性且具有口服活性的丙型肝炎病毒 (HCV) NS3/4A蛋白酶抑制剂,Ki值为 0.36 nM,并抑制 HCV 复制,EC50值为 7.8 nM。Simeprevir sodium 还能有效抑制SARS-CoV-2的复制,并与瑞德西韦 (Remdesivir) 具有协同作用。Simeprevir sodium 可抑制 SARS-CoV-2 的主要蛋白酶 (Mpro) 和 RNA 依赖性 RNA 聚合酶 (RdRp),并调节宿主免疫反应。
生物活性

Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specifichepatitis C virus (HCV) NS3/4A proteaseinhibitor with aKiof 0.36 nM. Simeprevir sodium inhibitsHCVreplication with anEC50of 7.8 nM. Simeprevir sodium also potently suppressesSARS-CoV-2replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].

IC50& Target

Ki: 0.36 nM (HCV NS3/4A protease)[1]
EC50: 7.8 nM (HCV replication)[1]
IC50: 9.6±2.3 μM (SARS-CoV-2 Mpro), 5.5±0.2 μM (SARS-CoV-2 RdRp)[4]

体外研究
(In Vitro)

Simeprevir (TMC435) inhibits HCV in a dose-dependent manner in Huh7-Luc cells, with EC50and EC90values of 8 nM and 24 nM, respectively[2].
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[3].
Simeprevir inhibits SARS-CoV-2 in Vero E6 cells with an IC50of 9.6±2.3 μM and 5.5±0.2 μM for Mproand RdRp, respectively[4].

体内研究
(In Vivo)

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.))[3].
Simeprevir (TMC435350) exhibits a medium-slow rate of absorption, well distribution with the high concentration observed in the liver, and a low clearance[1].
Pharmacokinetic Parameters of Simeprevir (TMC435350) in male Sprague-Dawley rats[1].

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[3]
Dosage:3 mg/kg
Administration:PO; single dosage
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 and 1409 ng·h/mL for rat and monkey, respectively.
Clinical Trial
Formula

C38H47N5NaO7S2

CAS 号

1241946-89-3

中文名称

西咪匹韦钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.