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> Sofosbuvir [1190307-88-0]

Sofosbuvir [1190307-88-0]

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Référence HY-15005-10mg

Conditionnement : 10mg

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Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM.

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Sofosbuvir Chemical Structure

Sofosbuvir Chemical Structure

CAS No. : 1190307-88-0

This product is a controlled substance and not for sale in your territory.

Based on 105 publication(s) in Google Scholar

Other Forms of Sofosbuvir:

  • PSI-7976 In-stock
  • Sofosbuvir impurity C In-stock
  • Sofosbuvir impurity A In-stock
  • Sofosbuvir-d6 In-stock
  • Enantiomer of Sofosbuvir In-stock
  • Sofosbuvir-13C,d3 Obtenir un devis

    Sofosbuvir purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    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.

    Sofosbuvir purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    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.

    Sofosbuvir purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2017;2017:1236801.  [Abstract]

    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.

    Sofosbuvir purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Nov 23;59(22):10268-10284.  [Abstract]

    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).
    Description

    Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM[1].

    IC50 & Target

    EC50: 92±5 nM (HCV)[1]
    In Vitro

    When cathepsin A (CatA) is incubated with PSI-7977 or Sofosbuvir (PSI-7977) for 150 min, ~18-fold more PSI-352707 is formed when Sofosbuvir (PSI-7977) is the substrate compared with PSI-7976. Moreover, the catalytic efficiency for Sofosbuvir (PSI-7977) with CatA is ~30-fold higher than that for PSI-7976[1]. The genotype coverage of Sofosbuvir (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, Sofosbuvir (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). Sofosbuvir (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, Sofosbuvir (PSI-7977) produces anti-HCV activity with EC90 values 0.42 μM[3].

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

    Sofosbuvir Related Antibodies
    Essai clinique
    Masse moléculaire

    529.45

    Formule

    C22H29FN3O9P
    CAS No.

    1190307-88-0
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@]1(F)[C@H](O)[C@@H](CO[P@](OC2=CC=CC=C2)(N[C@@H](C)C(OC(C)C)=O)=O)O[C@H]1N(C=CC(N3)=O)C3=O
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 50 mg/mL (94.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 25 mg/mL (47.22 mM; ultrasonic and warming and heat to 50°C)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Calculateur de molarité

    • Calculateur de dilution

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.67 mg/mL (3.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 4.55 mg/mL (8.59 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Pureté et documentation

    Purity: 99.97%

    COA (257 KB) RP-HPLC (276 KB)

    Instruction de manipulation (2659 KB)
    Références

    • [1]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47.  [Content Brief]

      [2]. Lam AM, et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68.  [Content Brief]

      [3]. Sofia MJ, et al. Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18.  [Content Brief]

      [4]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Content Brief]

    Test cellulaire
    [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 Sofosbuvir (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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Références

    • [1]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47.  [Content Brief]

      [2]. Lam AM, et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68.  [Content Brief]

      [3]. Sofia MJ, et al. Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18.  [Content Brief]

      [4]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Content Brief]

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.8888 mL 9.4438 mL 18.8875 mL 47.2188 mL
    5 mM 0.3778 mL 1.8888 mL 3.7775 mL 9.4438 mL
    10 mM 0.1889 mL 0.9444 mL 1.8888 mL 4.7219 mL
    15 mM 0.1259 mL 0.6296 mL 1.2592 mL 3.1479 mL
    20 mM 0.0944 mL 0.4722 mL 0.9444 mL 2.3609 mL
    25 mM 0.0756 mL 0.3778 mL 0.7555 mL 1.8888 mL
    30 mM 0.0630 mL 0.3148 mL 0.6296 mL 1.5740 mL
    40 mM 0.0472 mL 0.2361 mL 0.4722 mL 1.1805 mL
    DMSO 50 mM 0.0378 mL 0.1889 mL 0.3778 mL 0.9444 mL
    60 mM 0.0315 mL 0.1574 mL 0.3148 mL 0.7870 mL
    80 mM 0.0236 mL 0.1180 mL 0.2361 mL 0.5902 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Sofosbuvir Related Classifications

    Help & FAQs

    Keywords:

    Sofosbuvir1190307-88-0GS-7977 PSI-7977GS7977GS 7977PSI7977PSI 7977PSI-7977HCVHepatitis C virusInhibitorinhibitorinhibit

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