| Description | Ledipasvir (GS-5885) is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor. |
| In vitro | Ledipasvir针对GT1a和GT1b具有EC50值分别为31 pM和4 pM，经蛋白质调整后的EC50值分别为210 pM（GT1a）和27 pM（GT1b），其内在EC50值对于GT1a为310 fM，对GT1b为40 fM。Ledipasvir在人血清和含10% BSA的细胞培养基（复制子测定使用）中均高度蛋白质结合[1]。此外，Ledipasvir对JFH/3a-NS5A复制子展示出141 nM的EC50值[2]。 |
| In vivo | Ledipasvir不仅因其在复制子模型中的高效能而显著，也因其在大鼠、狗、猴体内具有低清除率、良好的生物利用度和长半衰期，以及在人类中预测的低清除率而受到关注。Ledipasvir的药代动力学在大鼠和狗中进行了测量，表现出在血浆中良好的半衰期（大鼠1.83 ± 0.22小时，狗2.63 ± 0.18小时）、低系统性清除率（CL）和中等分布体积（Vss），这些分布体积大于全身水分体积[1]。 |
| Target activity | NS5A (1a replicon):34 pM(EC50), NS5A (1b replicon):4 pM(EC50) |
| Synonyms | GS-5885, 雷迪帕韦 |
| molecular weight | 889 |
| Molecular formula | C49H54F2N8O6 |
| CAS | 1256388-51-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (104.6 mM) Ethanol: 93 mg/mL (104.6 mM) |
| References | 1. Link JO, 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, 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. |