1. Anti-infection Metabolic Enzyme/Protease
  2. Parasite Fungal Phosphatase Bacterial Antibiotic
  3. Pentamidine isethionate

Pentamidine isethionate  (Synonyms: MP-601205 isethionate)

Cat. No.: HY-B0537B Purity: 99.75%
COA Handling Instructions

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

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

Pentamidine isethionate Chemical Structure

Pentamidine isethionate Chemical Structure

CAS No. : 140-64-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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100 mg USD 40 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Pentamidine isethionate:

Top Publications Citing Use of Products

    Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: BMC Womens Health. 2022 Nov 24;22(1):470.  [Abstract]

    Pentamidine (2.5, 5 μM; 24-36 h) reduces cell migration in a dose- and time-dependent manner, in Ishikawa and HEC-1A cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].

    IC50 & Target

    Trypanosoma

     

    Leishmania

     

    In Vitro

    Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner[1].
    The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmania infantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein[2].

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

    Cell Viability Assay[1]

    Cell Line: WM9, DU145, C4-2, Hey, WM480, and A549 cells
    Concentration: 0-10 µg/mL
    Incubation Time: 6 days
    Result: The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 µg/mL.
    In Vivo

    Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice[1].

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

    Animal Model: Athymic nude mice (6 weeks old) injected with WM9 cells[1]
    Dosage: 0.25 mg/mouse
    Administration: Intramuscular injection; every 2 days; for 4 weeks
    Result: Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.
    Clinical Trial
    Molecular Weight

    592.68

    Formula

    C23H36N4O10S2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N=C(C1=CC=C(OCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.OCCS(=O)(O)=O.OCCS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (168.73 mM; Need ultrasonic)

    DMSO : 100 mg/mL (168.73 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 1.6873 mL 8.4363 mL 16.8725 mL
    5 mM 0.3375 mL 1.6873 mL 3.3745 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    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: ≥ 2.08 mg/mL (3.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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).
    Purity & Documentation

    Purity: 99.75%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.6873 mL 8.4363 mL 16.8725 mL 42.1813 mL
    5 mM 0.3375 mL 1.6873 mL 3.3745 mL 8.4363 mL
    10 mM 0.1687 mL 0.8436 mL 1.6873 mL 4.2181 mL
    15 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8121 mL
    20 mM 0.0844 mL 0.4218 mL 0.8436 mL 2.1091 mL
    25 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6873 mL
    30 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
    40 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0545 mL
    50 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8436 mL
    60 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
    80 mM 0.0211 mL 0.1055 mL 0.2109 mL 0.5273 mL
    100 mM 0.0169 mL 0.0844 mL 0.1687 mL 0.4218 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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    Pentamidine isethionate 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.

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