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Pibrentasvir

A hepatitis C virus NS5A inhibitor

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Pibrentasvir的二维码
  • 库存: 现货
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  • 5mg
    ¥625.00
    500.00
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  • 10mg
    ¥912.00
    730.00
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  • 25mg
    ¥1812.00
    1450.00
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  • 50mg
    ¥2887.00
    2310.00
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  • 100mg
    ¥4575.00
    3660.00
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  • 货号: ajci23150
  • CAS: 1353900-92-1
  • 别名: 哌仑他韦
  • 分子式: C57H65F5N10O8
  • 分子量: 1113.18
  • 纯度: >98%
  • 溶解度: DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml
  • 储存: Store at -20°C
  • 库存: 现货

Background

Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.


Pibrentasvir inhibits HCV genotype 1a-H77, 1b-Con1, and 2a-JFH-1 subgenomic replicons with 50% effective concentrations (EC50s) of 1.8, 4.3, and 5.0 pM, respectively. The antiviral activity of Pibrentasvir is attenuated 35- to 47-fold in the presence of 40% human plasma through sequestration of compound due to plasma protein binding. Pibrentasvir retains full activity against all of the genotype 1a and 1b single-position NS5A substitutions tested, except Y93H and Y93N in genotype 1a, which confers a ≤7-fold increase in EC50 to Pibrentasvir[1].


[1]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02558-16.

Protocol

Cell experiment:

The inhibitory effect of Pibrentasvir on HCV replication in replicon cells is determined in Dulbecco's modified Eagle's medium (DMEM) containing 5% fetal bovine serum with or without 40% human plasma. The cells are incubated with Pibrentasvir for 3 days and are subsequently lysed and processed according to the manufacturer's instructions to measure luciferase reporter activity using a Victor II luminometer. The 50% effective concentration (EC50) value is calculated using nonlinear regression curve fitting to the four-parameter logistic equation in software[1].

参考文献:

[1]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02558-16.

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