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R-7128

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Category Hepatitis C Virus (HCV)
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.
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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

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