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哌仑他韦(ABT-530) /Pibrentasvir {[allProObj[0].p_purity_real_show]}

货号:A275632 同义名: 哌仑他韦 / ABT-530

Pibrentasvir是一种蛋白酶抑制剂,潜在用于治疗 HCV(丙型肝炎病毒)感染。

Pibrentasvir 化学结构 CAS号:1353900-92-1
Pibrentasvir 化学结构
CAS号:1353900-92-1
Pibrentasvir 3D分子结构
CAS号:1353900-92-1
Pibrentasvir 化学结构 CAS号:1353900-92-1
Pibrentasvir 3D分子结构 CAS号:1353900-92-1
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Pibrentasvir 纯度/质量文件 产品仅供科研

货号:A275632 标准纯度: {[allProObj[0].p_purity_real_show]}
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Pibrentasvir 生物活性

描述 Hepatitis C virus (HCV) NS5A protein supports the replication of HCV by interacting with viral and cellular proteins to form the HCV replicase complex, the micro-organelle that replicates HCV RNA, thus making it an excellent target for the discovery of anti-HCV therapeutics. Pibrentasvir is a novel and pan-genotypic HCV NS5A inhibitor with EC50 values ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6. Pibrentasvir inhibited HCV genotype 1a-H77, 1b-Con1, and 2a-JFH-1 subgenomic replicons with EC50 values of 1.8, 4.3 and 5.0 pM, respectively; EC50 values ranged between 1.4 and 2.8 pM against chimeric stable replicons containing NS5A derived from HCV genotypes 2a, 2b, 3a, 4a, 5a, and 6a. The 50% cytotoxicity concentration (CC50) value of pibrentasvir in an HCV genotype 1a replicon cell line was > 32,000,000 pM, producing an in vitro therapeutic index that exceeded 107-fold. Furthermore, pibrentasvir retained full activity against all of the genotype 1a and 1b single-position NS5A substitutions tested, except Y93H and Y93N of genotype 1a, which conferred ≤ 7-fold increase in EC50 to pibrentasvir (EC50 ≤ 5.1 pM)[3].

Pibrentasvir 参考文献

[1]Gane E, Poordad F, et al. High Efficacy of ABT-493 and ABT-530 Treatment in Patients With HCV Genotype 1 or 3 Infection and Compensated Cirrhosis. Gastroenterology. 2016 Oct;151(4):651-659.e1.

[2]Lin CW, Dutta S, et al. Pharmacokinetics, Safety, and Tolerability Following Single and Multiple Doses of Pibrentasvir in a First-in-Human Study. Clin Pharmacol Drug Dev. 2017 May 2.

[3]Ng TI, Krishnan P, Pilot-Matias T, 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):e02558-16

Pibrentasvir 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.90mL

0.18mL

0.09mL

4.49mL

0.90mL

0.45mL

8.98mL

1.80mL

0.90mL

Pibrentasvir 技术信息

CAS号1353900-92-1
分子式C57H65F5N10O8
分子量 1113.18
别名 哌仑他韦 ;ABT-530
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 60 mg/mL(53.9 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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