Pibrentasvir
(Synonyms: 哌仑他韦) 目录号 : GC19454
A hepatitis C virus NS5A inhibitor
Cas No.:1353900-92-1
Sample solution is provided at 25 µL, 10mM.
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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.
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]. |
References: [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. | |
| Cas No. | 1353900-92-1 | SDF | |
| 别名 | 哌仑他韦 | ||
| Canonical SMILES | FC(C=C(N=C([C@H](CCC1)N1C([C@H]([C@@H](C)OC)NC(OC)=O)=O)N2)C2=C3)=C3[C@@H]4N(C5=CC(F)=C(N6CCC(C7=CC=C(F)C=C7)CC6)C(F)=C5)[C@@H](C(C=C(NC([C@H](CCC8)N8C([C@H]([C@@H](C)OC)NC(OC)=O)=O)=N9)C9=C%10)=C%10F)CC4 | ||
| 分子式 | C57H65F5N10O8 | 分子量 | 1113.18 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8983 mL | 4.4916 mL | 8.9833 mL |
| 5 mM | 0.1797 mL | 0.8983 mL | 1.7967 mL |
| 10 mM | 0.0898 mL | 0.4492 mL | 0.8983 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet