2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Protease HIV
  4. Nelfinavir Mesylate

Nelfinavir Mesylate  (Synonyms: AG 1343 Mesylate)

Cat. No.: HY-15287A Purity: 98.93%
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Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

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

Nelfinavir Mesylate Chemical Structure

Nelfinavir Mesylate Chemical Structure

CAS No. : 159989-65-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Nelfinavir Mesylate:

Nelfinavir Mesylate Related Antibodies

Top Publications Citing Use of Products

    Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Cells. 2022, 11(22), 3580

    Nelfinavir Mesylate (5 µM; 24 h) suppresses expression of MITF in A2058 and A375 cells.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent[1][2][3].

    IC50 & Target[1]

    HIV-1

     

    In Vitro

    Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells[4].
    Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells[4].
    Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines[4].
    Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4].
    Nelfinavir Mesylate activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system[4].
    Nelfinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 35.93 μM[5].

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

    Nelfinavir Mesylate Related Antibodies

    Cell Proliferation Assay[4]

    Cell Line: RPMI, LP1, U266, OPM2 and MM1S cells
    Concentration: 1, 2, 5, 10 μM
    Incubation Time: 48 hours
    Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 μM.

    Apoptosis Analysis[4]

    Cell Line: LP1 and U266 cells
    Concentration: 1-10 μM
    Incubation Time: 17 hours
    Result: Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+ cells.

    Western Blot Analysis[4]

    Cell Line: U266 cells
    Concentration: 5 μM
    Incubation Time: 0-24 hours
    Result: The level of AKT phosphorylation in U266 cells decreased.
    In Vivo

    Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice[4].

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

    Animal Model: NOD/SCID mice (bearing U266-luc cells)[4]
    Dosage: 75 mg/kg
    Administration: I.p.; 5 days a week for 21 days
    Result: Decreased MM cell growth in NOD/SCID mice.
    Clinical Trial
    Molecular Weight

    663.89

    Formula

    C33H49N3O7S2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    [H][C@]12C[C@@H](C(NC(C)(C)C)=O)N(C[C@H]([C@@H](NC(C3=C(C)C(O)=CC=C3)=O)CSC4=CC=CC=C4)O)C[C@@]1([H])CCCC2.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (150.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5063 mL 7.5314 mL 15.0627 mL
    5 mM 0.3013 mL 1.5063 mL 3.0125 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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: ≥ 5 mg/mL (7.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (7.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.93%

    SDS (393 KB)

    COA (262 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References

    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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5063 mL 7.5314 mL 15.0627 mL 37.6568 mL
    5 mM 0.3013 mL 1.5063 mL 3.0125 mL 7.5314 mL
    10 mM 0.1506 mL 0.7531 mL 1.5063 mL 3.7657 mL
    15 mM 0.1004 mL 0.5021 mL 1.0042 mL 2.5105 mL
    20 mM 0.0753 mL 0.3766 mL 0.7531 mL 1.8828 mL
    25 mM 0.0603 mL 0.3013 mL 0.6025 mL 1.5063 mL
    30 mM 0.0502 mL 0.2510 mL 0.5021 mL 1.2552 mL
    40 mM 0.0377 mL 0.1883 mL 0.3766 mL 0.9414 mL
    50 mM 0.0301 mL 0.1506 mL 0.3013 mL 0.7531 mL
    60 mM 0.0251 mL 0.1255 mL 0.2510 mL 0.6276 mL
    80 mM 0.0188 mL 0.0941 mL 0.1883 mL 0.4707 mL
    100 mM 0.0151 mL 0.0753 mL 0.1506 mL 0.3766 mL
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    Nelfinavir Mesylate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Nelfinavir159989-65-8AG 1343AG1343AG-1343HIV ProteaseHIVHuman immunodeficiency virusproteaseproliferationmultiplemyelomacellsphosphorylationNOproductioninfectionInhibitorinhibitorinhibit

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