Description
PSI-7977 is a phosphoramidate prodrug of PSI-7851.
Product Overview
PSI-7977 is a Nucleotide Inhibitor of Hepatitis C Virus. 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. 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 efficient replication and infection, and this particular isolate appeared to require additional amino acid changes together with S282T to reduce the activity of PSI-7977.
Synonyms
PSI 7977; sofosbuvir
Targets
HCV RNA-dependent RNA polymerase
Molecular Formula
C22H29FN3O9P
Chemical Name
propan-2-yl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request