Piroctone olamine [68890-66-4]

Cat# HY-B1345-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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Description

Piroctone olamine is a pyridine derivate. It is known to have a fungicidal effect.

IC50 & Target

Antifungal[1]

In Vitro

Piroctone olamine, the ethanolamine salt of the hydroxamic acid derivative Piroctone, is a hydroxypyridone anti-mycotic agent. Piroctone olamine penetrates the cell membrane and forms complexes with iron ions, inhibiting energy metabolism in mitochondria[1]. Piroctone olamine (PO) is an ethanolamine salt of the hydroxamic acid derivative Piroctone. All Candida strains show low minimum inhibitory concentrations (MICs) for Piroctone olamine (0.125-0.5 μg/mL) and Amphotericin B (AMB) (0.03-1 μg/mL)[2].

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

In Vivo

This work aimed to evaluate the antifungal activity of Piroctone olamine in the treatment of intra-abdominal candidiasis in an experimental model using Swiss mice. The treatment with Piroctone olamine (0.5 mg/kg) is performed 72 h after infection by intraperitoneal administration. For comparison, a group of animals (n=6) is treated with Amphotericin B (0.5 mg/kg). The mycological diagnosis is made by collecting the liver, spleen and kidneys. Data regarding the fungal growth and mortality are analyzed statistically by Student’s t test and analysis of variance, with level of significance set at P<0.05. The difference in fungal growth scoring between the control group and the treatment groups (Piroctone olamine and Amphotericin B) is statistically significant (P<0.05)[2].

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

Clinical Trial
Molecular Weight

298.42

Formula

C16H30N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(C)C=C(CC(C)CC(C)(C)C)N1O.NCCO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (167.55 mM; ultrasonic and adjust pH to 9 with NaOH)

DMSO : 11.11 mg/mL (37.23 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 3.3510 mL 16.7549 mL 33.5098 mL
5 mM 0.6702 mL 3.3510 mL 6.7020 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). 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.

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: ≥ 1.11 mg/mL (3.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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: ≥ 1.11 mg/mL (3.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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
References

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