Ledipasvir

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Chemical Structure| 1256388-51-8 同义名 : GS-5885
CAS号 : 1256388-51-8
货号 : A150793
分子式 : C49H54F2N8O6
纯度 : 99%
分子量 : 889.0
MDL号 : MFCD25976756
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(56.24 mM)，配合低频超声助溶，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
靶点

  • HCV Protease
描述 Hepatitis C virus (HCV) infection is a significant public health concern and is the leading cause of liver transplant and hepatocellular carcinoma. The NS5A polymerase is critical for HCV viability. Ledipasvir is a potent and selective HCV NS5A inhibitor. Ledipasvir has GT1a and 1b EC50 values of 31 and 4 pM, respectively, and protein-adjusted EC50 values of 210 pM (GT1a) and 27 pM (GT1b). Ledipasvir is remarkable on the basis of its low clearance, good bioavailability, and long half-lives (4.7−10.3 h) in rat, dog, and monkey and low predicted clearance in human (0.012 L/h/kg)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.62mL

1.12mL

0.56mL

11.25mL

2.25mL

1.12mL
参考文献

[1]Link JO, Taylor JG, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46.

[2]Hernandez D, Zhou N, et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013 May;57(1):13-8.

[3]Link JO, Taylor JG, Xu L, Mitchell M, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46