Danoprevir

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Chemical Structure| 850876-88-9 同义名 : ITMN-191; R7227; RG7227; RO5190591
CAS号 : 850876-88-9
货号 : A226220
分子式 : C35H46FN5O9S
纯度 : 99%+
分子量 : 731.83
MDL号 : MFCD16038038
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • HCV Protease

    HCV NS3/4A protease, IC50:0.2 nM-3.5 nM

  • HCV Protease

    HCV NS3/4A protease, IC50:0.2 nM-3.5 nM
描述 The NS3 protein is a chymotrypsin-like serine protease that is activated by association with NS4A. NS3/4A (nonstructural protein 3/4A) liberates the functional form of the viral polymerase and other viral proteins required for HCV replication. Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of HCV with an IC50 rang of 0.2 - 3.5 nM. In peptide cleavage assays, danoprevir reduced genotype 1b NS3/4A protease activity in a concentration-dependent fashion. Dose-dependent reductions of a patient-derived HCV genotype 1b replicon harbored in hepatocyte-derived Huh7 cells were observed following 2-day incubation with danoprevir. In any case, treatment with 45 nM danoprevir (3 times its EC90) reduced HCV replicon RNA levels below the RT-PCR detection limit in a sustained fashion and completely cleared replicon RNA. In monkey liver tissue, the maximum concentration in the liver (Cmax) and the 12-h-postdose concentration in the liver (C12 h) were sufficient to reduce HCV replicon RNA by 3.1 log10 and 2.0 log10 units, respectively[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.37mL

0.27mL

0.14mL

6.83mL

1.37mL

0.68mL

13.66mL

2.73mL

1.37mL
参考文献

[1]Seiwert SD, Andrews SW, et al. Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227). Antimicrob Agents Chemother. 2008 Dec;52(12):4432-41.

[2]Bartels DJ, Zhou Y, et al. Natural prevalence of hepatitis C virus variants with decreased sensitivity to NS3.4A protease inhibitors in treatment-naive subjects. J Infect Dis. 2008 Sep 15;198(6):800-7.

[3]Seiwert SD, Andrews SW, et al. Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227). Antimicrob Agents Chemother. 2008 Dec;52(12):4432-41