1. Anti-infection
  2. HCV

PSI-7977 (Synonyms: GS 7977; sofosbuvir)

Cat. No.: HY-15005 Purity: 99.95%
Handling Instructions

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

For research use only. We do not sell to patients.

PSI-7977 Chemical Structure

PSI-7977 Chemical Structure

CAS No. : 1190307-88-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 105 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 174 In-stock
Estimated Time of Arrival: December 31
100 mg USD 216 In-stock
Estimated Time of Arrival: December 31
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Other Forms of PSI-7977:

Customer Validation

    PSI-7977 purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor emtricitabine). Results are representative of 4 independent experiments.

    PSI-7977 purchased from MCE. Usage Cited in: Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.

    Simeprevir inhibits DNA damage repair following irradiation. U251, BT474, and HepG2 cells are pretreated with Simeprevir or DMSO and irradiated at a dose of 6 Gy. After 6 hours, prolongation of γH2AX foci is detected in Simeprevir-treated cells along with decreased phosphorylation of DNA-PKcs, indicating impaired nonhomologous end-joining repair.

    PSI-7977 purchased from MCE. Usage Cited in: J Med Chem. 2016 Nov 23;59(22):10268-10284.

    Huh7.5 cells are infected with HCV (45 IU/cell) and simultaneously treated with Simeprevir (A, 0.025 μM), Sofosbuvir (B, 0.1 μM), or Daclatasvir (C, 16 pM) alone or with 1 (6.25 μM).

    PSI-7977 purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1236801.

    Huh7.5 (HCV+) cells are treated with 1 μM of Simeprevir or solvent control. At 24 hours, the cells are washed and continuously incubated with fresh culture media containing drugs again for 48 hours. The cultural supernatants are then harvested and directly incubated to naïve Huh7.5 cells. After been passaged 1~3 times, the newly infected cells are treated with 1 μM of Simeprevir for 72 hours. Intracellular proteins are extracted and detected with WB.

    PSI-7977 purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1236801.

    Huh7.5 (HCV+) cells are treated with 1 μM of Sofosbuvir or solvent control. At 24 hours, the cells are washed and continuously incubated with fresh culture media containing drugs again for 48 hours. The cultural supernatants are then harvested and directly incubated to naïve Huh7.5 cells. After been passaged 1~3 times, the newly infected cells are treated with 1 μM of Sofosbuvir for 72 hours. Intracellular proteins are extracted and detected with WB.

    PSI-7977 purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1236801.

    Naïve Huh7.5 cells are infected with wild and mutant type HCV and simultaneously treated with drugs. Intracellular proteins were extracted and detected with WB in 72 hours. Telaprevir (VX-950) against WT and A156T mutant HCV.

    PSI-7977 purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.

    GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), Sofosbuvir (0.8 μM), Daclatasvir (0.15 μM) or solvent control for 6 days.

    PSI-7977 purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.

    Huh7.5 cells are infected with HCV and simultaneously treated with 7f (10 μM) or DAA (0.04 μM Simeprevir, 0.08 μM Sofosbuvir, or 16 pM Daclatasvir) or 7f plus DAA.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    EC50: 92±5 nM (HCV)[1]

    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].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8888 mL 9.4438 mL 18.8875 mL
    5 mM 0.3778 mL 1.8888 mL 3.7775 mL
    10 mM 0.1889 mL 0.9444 mL 1.8888 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Sofosbuvir is prepared in vehicle (ddH2O)[4].

    References
    Cell Assay
    [1]

    Clone A cells are seeded into T75 flasks at about 5×106 cells/flask in Dulbecco's modified Eagle's medium (DMEM) containing 100 IU/mL Penicillin/100 μg/mL streptomycin and 10% fetal bovine serum. Similarly, human primary hepatocytes are seeded in cell plating medium into T75 flasks at about 5×106 cells/flask. After overnight incubation to allow the cells to attach, cells are incubated with 50 μM PSI-7851, PSI-7976, or PSI-7977 in fresh medium for clone A cells or in cell maintenance medium for primary hepatocytes for up to 24 h at 37°C in a 5% CO2 atmosphere. The same procedures are applied when radiolabeled PSI-7851 is used in the study except that 1×106 cells per well are seeded into a 6-well plate, and the cells are incubated with 5 μM [3H]PSI-7851. At selected times, the medium is removed, and the cell layer is washed with cold phosphate-buffered saline (PBS). After trypsinization, cells are counted and centrifuged at 1,200 rpm for 5 min. The cell pellets are suspended in 1 mL of cold 60% methanol and incubated overnight at −20°C. The samples are centrifuged at 14,000 rpm for 5 min, and the supernatants are collected and dried using a SpeedVac concentrator and stored at −20°C until they are analyzed by high performance liquid chromatography (HPLC). Residues are suspended in 100 μL of water, and 50-μL aliquots are injected into HPLC[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    529.45

    Formula

    C₂₂H₂₉FN₃O₉P

    CAS No.

    1190307-88-0

    SMILES

    O=C1N([[email protected]]2[[email protected]]([[email protected]](O)[[email protected]@H](CO[[email protected]](OC3=CC=CC=C3)(N[[email protected]@H](C)C(OC(C)C)=O)=O)O2)(C)F)C=CC(N1)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.95%

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    Product Name:
    PSI-7977
    Cat. No.:
    HY-15005
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    PSI-7977

    Cat. No.: HY-15005