1. Metabolic Enzyme/Protease
    Anti-infection
  2. HCV Protease
    HCV

R-7128 (Synonyms: RG 7128; Mericitabine; PSI 6130 diisobutyrate)

Cat. No.: HY-10240 Purity: 99.34%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
R-7128 Chemical Structure

R-7128 Chemical Structure

CAS No. : 940908-79-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $248 In-stock
5 mg $225 In-stock
10 mg $306 In-stock
50 mg $799 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

HCV NS5B polymerase[1]

In Vitro

R-7128 (Mericitabine) 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. 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. R-7128 demonstrates a relatively good safety profile and significant potency against HCV-1[2]. R-7128 (Mericitabine, RG7128) 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[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01482403 Hoffmann-La Roche Hepatitis C, Chronic November 2011 Phase 2
NCT01482390 Hoffmann-La Roche Hepatitis C November 30, 2011 Phase 2
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References
Molecular Weight

399.41

Formula

C₁₈H₂₆FN₃O₆

CAS No.

940908-79-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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R-7128
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HY-10240
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