PSI-7977

Short Summary : Antiviral agents for chronic HCV infection

Category : DNA Damage/DNA Repair|DNA Synthesis

Purity : 0.9986

CAS Number : 1190307-88-0

Formula : C22H29FN3O9P

Molecular Weight : 529.45

SMILE : CC(C)OC(=O)C(C)NP(=O)(OCC1C(C(C(O1)N2C=CC(=O)NC2=O)(C)F)O)OC3=CC=CC=C3

Solubility : >183mg/mL in DMSO

Storage : Store at -20°C

Description : PSI-7977 is a Nucleotide Inhibitor of Hepatitis C Virus [2]Hepatitis C virus (HCV) is a disease of liver cirrhosis and development of cancer in liver (hepatocellular carcinoma).Results from studies using GT 1a (H77)-, 1b (Con1)-, and 2a (JFH-1)-derived replicons and chimeric replicons with the NS5B region fromGT 2a (J6), 2b, and 3a clearly showed that PSI-7977 is a potent HCV inhibitor across NS5B proteins from different isolates. PSI-7977 inhibited the enzymatic activity of NS5B polymerase from GTs 1 to 4 with similar 50% inhibitory concentrations [1]. PSI-7977 is a potent HCV inhibitor with broad genotype coverage. Cross-resistance and selection studies showed that S282T is likely the amino acid change that will be selected by PSI-7977 across various genotypes and subtypes. JFH-1 is a highly unique strain capable of ef cient replication and infection, and this particular isolate appeared to require additional amino acid changes together with S282T to reduce the activity of PSI-7977. [3]References:[1] Lam AM, Murakami E, Espiritu C et al. PSI-7851, a pronucleotide of beta-D-2′-deoxy-2′-fluoro-2′-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96.[2] Abdo A. Elfiky, Wael M. Elshemey , Wissam A. Gawad , Omar S. Desoky Molecular Modeling Comparison of the Performance of NS5b Polymerase Inhibitor (PSI-7977) on Prevalent HCV Genotypes. Protein J (2013) 32:75–80.[3] Angela M. Lam, Christine Espiritu, Shalini Bansal et al. Genotype and Subtype Profiling of PSI-7977 as a Nucleotide Inhibitor of Hepatitis C Virus. Antimicrobial Agents and Chemotherapy June 2012 Volume 56 Number 6 p 3359–3368.

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