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Antiviral API
- Arenavirus
- Cytomegalovirus (CMV)
- Dengue virus
- Endogenous Metabolite
- Enterovirus (EV)
- Epstein-Barr virus (EBV)
- Filovirus
- Flavivirus
- HCV Protease
- Hepatitis B Virus (HBV)
- Hepatitis C Virus (HCV)
- Herpes simplex Virus (HSV)
- HIF/HIF Prolyl-Hydroxylase
- HIV Integrase
- HIV Protease
- Human immunodeficiency Virus (HIV)
- Human papillomavirus (HPV)
- Influenza Virus
- Nipah virus
- Orthopoxvirus
- Others
- Rabies virus (RABV)
- Respiratory syncytial Virus (RSV)
- Reverse Transcriptases (RTs)
- SARS-CoV
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- Virus Protease
- West Nile virus
- Antiviral intermediates
Mericitabine
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| Category | HCV Protease |
| CAS | 940908-79-2 |
| Description | R-7128 is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, with activity across all HCV genotypes. It is a nucleoside polymerase inhibitor (NPI) and is able to inhibit the RNA synthesis of HCV in vitro. |
Product Information
| Synonyms | R 7128; R-7128; R7128; RG7128; RG 7128; RG-7128; PSI 6130 diisobutyrate; RO-5024048; 3',5'-Diisobutyryl PSI 6130; 2'-Deoxy-2'-fluoro-2'-C-methylcytidine diisobutyrate |
| IUPAC Name | [(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-fluoro-4-methyl-3-(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate |
| Molecular Weight | 399.41 |
| Molecular Formula | C18H26FN3O6 |
| Canonical SMILES | CC(C)C(=O)OCC1C(C(C(O1)N2C=CC(=NC2=O)N)(C)F)OC(=O)C(C)C |
| InChI | InChI=1S/C18H26FN3O6/c1-9(2)14(23)26-8-11-13(28-15(24)10(3)4)18(5,19)16(27-11)22-7-6-12(20)21-17(22)25/h6-7,9-11,13,16H,8H2,1-5H3,(H2,20,21,25)/t11-,13-,16-,18-/m1/s1 |
| InChIKey | MLESJYFEMSJZLZ-MAAOGQSESA-N |
| Boiling Point | 496.1±55.0 °C (Predicted) |
| Purity | 98% |
| Density | 1.36 g/cm3 |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | White to Off-white Solid |
| Storage | Store at -20 °C |
| Complexity | 707 |
| Exact Mass | 399.18056372 |
| In Vitro | Mericitabine (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 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 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. R-7128 is an oral cytidine nucleoside analog prodrug that exhibits strong antiviral effectiveness against the HCV polymerase across all HCV genotypes. |
| PSA | 123.73000 |
| Target | HCV NS5B polymerase |
| XLogP3-AA | 1.3 |
