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Mericitabine

Cat. No. M30944
Mericitabine Structure
Synonym:

RG 7128; R-7128; PSI 6130 diisobutyrate

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Biological Activity

Mericitabine (RG 7128; 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.

Chemical Information
Molecular Weight 399.41
Formula C18H26FN3O6
CAS Number 940908-79-2
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ya-Chi Chen, et al. Clin Pharmacol Drug Dev. Evaluation of the effect of mericitabine at projected therapeutic and supratherapeutic doses on cardiac repolarization in healthy subjects: A thorough QT/QTc study

[2] Heiner Wedemeyer, et al. PLoS One. Mericitabine and Either Boceprevir or Telaprevir in Combination with Peginterferon Alfa-2a plus Ribavirin for Patients with Chronic Hepatitis C Genotype 1 Infection and Prior Null Response: The Randomized DYNAMO 1 and DYNAMO 2 Studies

[3] Laetitia Canini, et al. Antivir Ther. Modelling the interaction between danoprevir and mericitabine in the treatment of chronic HCV infection

[4] Edward J Gane, et al. Liver Int. Mericitabine and ritonavir-boosted danoprevir with or without ribavirin in treatment-naive HCV genotype 1 patients: INFORM-SVR study

[5] Jean-Michel Pawlotsky, et al. Antivir Ther. Resistance to mericitabine, a nucleoside analogue inhibitor of HCV RNA-dependent RNA polymerase

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Keywords: Mericitabine, RG 7128; R-7128; PSI 6130 diisobutyrate supplier, Anti-infection, inhibitors, activators

 
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