PSI-6206
PSI-6206 (as known as RO-2433 or GS-331007), β-D-2’-deoxy-2’-fluoro-2’-C-methyluridine, is the deaminated derivative of PSI-6130, β-D-2’-deoxy-2’-fluoro-2’-C-methylcytidine, which is a potent inhibitor of hepatitis C virus (HCV) replication in the subgenomic HCV reolicon system. PSI-6206, itself, does not shown any inhibitory activity towards HCV replication in the HCV subgenomic replicon system. However, the its triphosphate form, RO2433-TP, is a potent inhibitor of RNA synthesis by HCV polymerase, which inhibits both the RNA sysnthesis activity of HCV replicase (IC50 = 1.19 uM) and the RNA synthesis activity of the recombinant HCV Con1 NS58 on a heteropolymeric RNA template derived from the 3’-end of the negative strand of the HCV genome (IC50 = 0.52 uM and Ki = 0.141 uM).
Reference
Han Ma, Wen-Rong Jiang, Nicole Robledo, Vincent Leveque, Samir Ali, Teresa Lara-Jamie, Mohammad Masjedizadeh, David B. Smith, Nick Cammack, Klaus Klumpp, and Julian Symons. Characterization of the metabolic ctivation of hepatitis C virus nucleoside inhibitor β-D-2’-deoxy-2’-fluoro-2’-C-methylcytidine (PSI-6130) and identification of a novel active 5’-triphosphate species. The Journal of Biological Chemistry 2007; 282(41): 29812-29820
- 1. Eyer L, ?mídková M, et al. "Structure-activity relationships of nucleoside analogues for inhibition of tick-borne encephalitis virus. Antiviral Res." 2016 Jul 28;133:119-129. PMID:27476046
- 2. Eyer L, Nencka R, et al. "Nucleoside inhibitors of Zika virus." J Infect Dis. 2016 May 27. pii:jiw226. PMID:27234417
- 3. Rower, Joseph E, et al. "Validation and application of an LC-MS/MS method to determine the concentrations of sofosbuvir anabolites in cells." Antimicrobial agents and chemotherapy (2015): AAC-01693. PMID:26416874
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 260.22 |
Cas No. | 863329-66-2 |
Formula | C10H13FN2O5 |
Solubility | ≥13.1 mg/mL in DMSO; ≥24.15 mg/mL in EtOH with ultrasonic; ≥48.7 mg/mL in H2O with ultrasonic |
Chemical Name | 1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione |
SDF | Download SDF |
Canonical SMILES | CC1(C(C(OC1N2C=CC(=O)NC2=O)CO)O)F |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | PSI-6206 (RO2433) is a selective inhibitor of HCV RNA polymerase . | |||||
Targets | HCV | |||||
IC50 |
Quality Control & MSDS
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