Mericitabine

SKU: orb1307815

Description

Mericitabine (R-7128) is a nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. It functions as a chain terminator, halting viral genome replication. This inhibitor has been utilized in both in vitro enzymatic assays and in vivo animal models to study HCV replication mechanisms and antiviral strategies.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 940908-79-2
• MW: 399.41
• Purity: 98.54% (May vary between batches)
• Formula: C₁₈H₂₆FN₃O₆
• SMILES: CC(C)C(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)[C@](C)(F)[C@@H]1OC(=O)C(C)C
• Target: HCV Protease
• Solubility: DMSO:100 mg/mL (250.37 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.01 mM)

Bioactivity

• In Vitro:
  PSI-6130 is converted through phosphorylation by cellular kinases to an active 5′-triphosphate metabolite, which inhibits the NS5B RNA polymerase of HCV. Mericitabine is an oral cytidine nucleoside analog prodrug that exhibits strong antiviral effectiveness against the HCV polymerase across all HCV genotypes. Mericitabine is a first-in-class nucleoside polymerase inhibitor (NPI), which requires intracellular uptake and phosphorylation to two active triphosphates. Mericitabine, a cytidine analogue, is an oral prodrug of PSI-6130. PSI-6130 has an EC90 value of 4.6±2 μM in the HCV replicon assay. Mericitabine displays high specificity for HCV, minimal cytotoxicity, and does not affect mitochondrial DNA. Mericitabine shows a relatively good safety profile and significant potency against HCV-1 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

R 7128, R7128, R-7128, PSI6130, PSI-6130, PSI6130 Diisobutyrate, PSI-6130 Diisobutyrate, PSI 6130, PSI 6130 Diisobutyrate, PSI 6130 diisobutyrate, RG 7128, RG7128, RG-7128, Inhibitor, HCVProtease, HCV Protease, HCV NS5B polymerase, HCV, Hepatitis C virus, inhibit, Mericitabine

Compound Identifiers

PubChem CID

16122663