Pibrentasvir

产品说明书

Print
Chemical Structure| 1353900-92-1 同义名 : 哌仑他韦 ;ABT-530
CAS号 : 1353900-92-1
货号 : A275632
分子式 : C57H65F5N10O8
纯度 : 99%+
分子量 : 1113.18
MDL号 : MFCD30747902
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 :

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

动物实验配方:
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].
实验方案
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

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