Name | PSI 7977 |
Synonyms | GS 7977 GS-7977 Psi-7977 PSI-7977 PSI 7977 Sofosbuvir SOFOSBUVIR sovaldi API Sophy Bouvet sofosbuvir form6 sofosvuvir form6 Sofosbuvir1190307-88-0 PSI-7977 Discontinued Sofosbuvir and intermediates L-Alanine, N-[[p(S),2'R]-2'-deoxy-2'-fluoro-2'-methyl-p-phenyl-5'-uridylyl]-, 1-methylethyl ester L-Alanine, N-[[P(S),2'R]-2'-deoxy-2'-fluoro-2'-Methyl-P-phenyl-5'-uridylyl]-, 1-Methylethyl ester (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyriMidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-Methyltetrahydrofuran-2-yl)Methoxy)(phenoxy)phosphoryl)aMino)propanoate (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate Isopropyl (2S)-2-{[(S)-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl)-4-fluoro-3-hydroxy-4-methyltetrahydro-2-furanyl]methoxy}(phenoxy)phosphoryl]amino}propanoate |
CAS | 1190307-88-0 1064684-44-1 |
EINECS | 695-717-4 |
Molecular Formula | C22H29FN3O9P |
Molar Mass | 529.45 |
Density | 1.41 |
Melting Point | 122-124°C |
Solubility | DMSO |
Appearance | Solid |
Color | White |
pKa | 9.39±0.10(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
In vitro study | As a HCV NS5B polymerase inhibitor, PSI-7977 inhibited HCV RNA replication more effectively than PSI-7976, with EC50 of 92 nM and 1.07 μm, respectively, EC90 is 0.29 μm and 2.99 μm respectively. Correspondingly, clone A cells are incubated with PSI-7977, which is better than clone A cells incubated with PSI-7976, higher concentrations of PSI-7409 were produced. PSI-7977 is an effective substrate for CatA, forming PSI-352707, which is more than 30 times more effective than PSI-7976. The S282T NS5B polymerase mutant but not the S96T mutant was resistant to PSI-7977, and EC90 was increased from 0.42 μm to 7.8 μm. In the 8-day cytotoxicity assay, PSI-7977 was not toxic to Huh7, HepG2, BxPC3, and CEM cells, even at concentrations as high as 100 μm. PSI-7977 treatment of HepG2 cells for 14 days inhibited mtDNA and rDNA with IC90 of 72.1 μm and 68.6 μm, respectively. PSI-7977 potently inhibited replication of genotypes (GT) 1a, 1b, and 2a, as well as chimeric replication containing GT 2a, 2b, and 3a NS5B polymerases. JFH-1 sequence analysis of the NS5B region illustrates the selection of other amino acid changes before and after the appearance of S282T, including T179A, M289L, I293L, M434T, and H479P, required to resist PSI-7977. |
HS Code | 29339900 |