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
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 174 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 216 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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: 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
    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [1]

    PSI-7977 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[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

    Solvent & Solubility

    10 mM in DMSO

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

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.95%

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

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