| Description | Mericitabine (R-7128) is a nucleoside HCV NS5B polymerase inhibitor. It acts as an RNA chain terminator and prevents the elongation of RNA transcripts during replication. |
| In vitro | PSI-6130 在细胞激酶的作用下通过磷酸化转化为活性的5′-三磷酸代谢物，从而抑制HCV的NS5B RNA聚合酶。Mericitabine 是一种口服的胞苷核苷类似物前体药，对所有HCV基因型的HCV聚合酶展示出强大的抗病毒效力。Mericitabine是首创的核苷聚合酶抑制剂(NPI)，需在细胞内摄取并磷酸化为两个活性的三磷酸。Mericitabine, 作为一种胞苷类似物，是PSI-6130的口服前体药。PSI-6130在HCV复制子测定中的EC90值为4.6±2 μM。Mericitabine对HCV具有高度特异性，最小细胞毒性，并不影响线粒体DNA。Mericitabine表现出相对良好的安全性和针对HCV-1的显著效力[2][3]。 |
| Synonyms | R-7128, RG 7128, PSI 6130 diisobutyrate |
| molecular weight | 399.41 |
| Molecular formula | C18H26FN3O6 |
| CAS | 940908-79-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (250.37 mM), Sonication is recommended. |
| References | 1. Le Pogam S, et al. Characterization of HCV quasispecies dynamics upon short term dual-therapy with the HCV NS5B nucleoside polymerase inhibitor mericitabine and the NS3/4 protease inhibitor danoprevir. Antimicrob Agents Chemother. 2012 Nov;56(11):5494-5 2. Soriano V, et al. Directly acting antivirals against hepatitis C virus. J Antimicrob Chemother. 2011 Aug;66(8):1673-86 3. Guedj J, et al. Hepatitis C viral kinetics with the nucleoside polymerase inhibitor mericitabine (RG7128). Hepatology. 2012 Apr;55(4):1030-7. |