Sofosbuvir, NS5B polymerase inhibitor

PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

Product information

CAS Number: 1190307-88-0

Molecular Weight: 529.45

Formula: C22H29FN3O9P

Synonym:

Sovaldi

Virunon

Vosevi

Hepcinat

Hepcvir

Resof

GS-7977

PSI-7977

Chemical Name: propan-2-yl (2S)-2-{[(S)-{[(2R, 3R, 4R, 5R)-5-(2, 4-dioxo-1, 2, 3, 4-tetrahydropyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy}(phenoxy)phosphoryl]amino}propanoate

Smiles: CC(C)OC(=O)[C@H](C)N[P@](=O)(OC[C@H]1O[C@@H](N2C=CC(=O)NC2=O)[C@](C)(F)[C@@H]1O)OC1=CC=CC=C1

InChiKey: TTZHDVOVKQGIBA-IQWMDFIBSA-N

InChi: InChI=1S/C22H29FN3O9P/c1-13(2)33-19(29)14(3)25-36(31,35-15-8-6-5-7-9-15)32-12-16-18(28)22(4,23)20(34-16)26-11-10-17(27)24-21(26)30/h5-11,13-14,16,18,20,28H,12H2,1-4H3,(H,25,31)(H,24,27,30)/t14-,16+,18+,20+,22+,36-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: 10 mM in DMSO Sofosbuvir is prepared in vehicle (ddH2O)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

When cathepsin A (CatA) is incubated with PSI-7977 or PSI-7976 for 150 min, ~18-fold more PSI-352707 is formed when PSI-7977 is the substrate compared with PSI-7976. Moreover, the catalytic efficiency for PSI-7977 with CatA is ~30-fold higher than that for PSI-7976[1]. The genotype coverage of PSI-7977 by using GT 1b (Con1)-, 1a (H77)-, and 2a (JFH-1)-derived replicons and GT 1b chimeric replicons containing the NS5B region from the J6 GT 2a isolate and from GT 2b and GT 3a patient isolates is evaluated, PSI-7977 inhibits the replication of these replicons with similar EC50s (between 16 and 48 nM), and is especially active against the chimeric replicon containing the J6 NS5B (EC50=4.7 nM). PSI-7977 inhibits clone A (GT 1b) wild-type and S282T replicons with EC90 values of 0.42 and 7.8 μM, respectively[2]. In the clone A replicon assay, PSI-7977 produces anti-HCV activity with EC90 values 0.42 μM[3].

References:

1. Murakami E, et al. J Biol Chem, 2010, 285(45), 34337-34347.
2. Sofia MJ, et al. J Med Chem, 2010, 53(19), 7202-7218.
3. Lam AM, et al. Antimicrob Agents Chemother, 2012, 56(6), 3359-3368.

Products are for research use only. Not for human use.