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Antiviral API
- Arenavirus
- Cytomegalovirus (CMV)
- Endogenous Metabolite
- Enterovirus (EV)
- Epstein-Barr virus (EBV)
- Filovirus
- 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
- Orthopoxvirus
- Others
- Respiratory syncytial Virus (RSV)
- Reverse Transcriptases (RTs)
- SARS-CoV
- Virus Protease
- Antiviral intermediates
R-7128
Category | Virus 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 | Mericitabine; PSI 6130 diisobutyrate; RG7128; RG-7128; RG 7128; R-7128; R7128; R 7128; PSI 6130 diisobutyrate; 3',5'-Diisobutyryl PSI 6130; Mericitabine |
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 |
Purity | >98% |
Solubility | In vitro: 10 mM in DMSO |
Appearance | White to off-white (Solid) |
Storage | Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month |
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 |