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PSI-6206 (RO2433) is the unphosphorylated parent compound of triphosphate analog PSI-7409, which is a potent inhibitor of the HCV NS5B RNA dependent RNA polymerase. The monophosphate form of PSI-6206 was shown to be metabolized in primary human hepatocytes to its triphosphate analog PSI-7409. Furthermore, the phosphoramidate prodrug of PSI-6206 monophosphate, PSI-7851, was developed. Alternatively, PSI-6130, an aminated analog of PSI-6206 monophosphate, was also developed. (1,2,3)
PSI-7409, the triphosphate of PSI-6206 inhibits wild-type and S282T HCV RdRp with Ki values of 0.42 and 22 uM, respectively. PSI-7851, the phosphoramidate of PSI-6206 monophosphate, showed an EC50 value of 1.62 uM for inhibiting HCV RNA replication. (2)
Technical information:
| Chemical Formula: | C10H13FN2O5 | |
| CAS #: | 863329-66-2 | |
| Molecular Weight: | 260.22 | |
| Purity: | > 98% | |
| Appearance: | Clear Crystal | |
| Chemical Name: | (2R)-2-Deoxy-2-fluoro-2-methyluridine | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | PSI-6206, RO-2433, PSI6206, RO2433 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Rodriguez-Torres et al., Antiviral Activity, Pharmacokinetics, Safety, and Tolerability of PSI-7851, a Novel Nucleotide Polymerase Inhibitor for HCV, Following Single and 3 Day Multiple Ascending Oral Doses in Healthy Volunteers and Patients with Chronic HCV Infection. 60th AASLD Annual Meeting, 2009. |
| 2. | Murakami et al., The Mechanism of Action of b-D-2-Deoxy-2-Fluoro-2-C-Methylcytidine Involves a Second Metabolic Pathway Leading to b-D-2-Deoxy-2-Fluoro-2-C-Methyluridine 5-Triphosphate, a Potent Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase. Antimicrob. Agents. Chemother. 2008, 52(2), 458-464. Pubmed ID: 17999967 |
| 3. | Ma et al., Characterization of the Metabolic Activation of Hepatitis C Virus Nucleoside Inhibitor b-D-2-Deoxy-2-fluoro-2-C-methylcytidine (PSI-6130) and Identification of a Novel Active 5-Triphosphate Species. J. Biol. Chem. 2007, 282, 29812-29820. Pubmed ID: 17698842 |