| 产品描述： | Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication. |
| 靶点： |
HCV NS5B polymerase;HCVProtease |
| 体外研究： |
Mericitabine (RG 7128; R-7128) is an oral prodrug of PSI-6130, a cytidine analogue. Pre-clinical observations demonstrated that PSI-6130 has an EC90 value of 4.6±2 μM in the HCV replicon assay. Mericitabine (RG 7128; R-7128) shows high specificity for HCV, minimal cytotoxicity and does not affect mitochondrial DNA. PSI-6130 is converted through phosphorylation by cellular kinases to an active 5′-triphosphate metabolite, which inhibits the NS5B RNA polymerase of HCV. Mericitabine (RG 7128; R-7128) demonstrates a relatively good safety profile and significant potency against HCV-1. Mericitabine is a first-in class nucleoside polymerase inhibitor (NPI), which requires intracellular uptake and phosphorylation to two active triphosphates.Mericitabine (RG 7128; R-7128) is an oral cytidine nucleoside analog prodrug that exhibits strong antiviral effectiveness against the HCV polymerase across all HCV genotypes |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.504 ml |
12.518 ml |
25.037 ml |
| 5 mM |
0.501 ml |
2.504 ml |
5.007 ml |
| 10 mM |
0.25 ml |
1.252 ml |
2.504 ml |
| 50 mM |
0.05 ml |
0.25 ml |
0.501 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京