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PF-1163A

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Catalog No. TN7560Cas No. 258871-59-9

PF-1163A, a depsipeptide antifungal compound isolated from Penicillium, blocks ergosterol synthesis with an IC50 of 12 ng/ml. This compound specifically inhibits the enzyme ERG25p, a C-4 methyl oxidase in the ergosterol biosynthetic pathway, leading to its antifungal activity. Notably, in Saccharomyces cerevisiae modified to express ERG biosynthesis genes, PF-1163A exhibits an inhibition concentration (MIC value) of 12.5 µg/ml against ERG25p, though strains overexpressing ERG25p show resistance. Additionally, PF-1163A effectively suppresses the growth of Candida albicans (MIC = 8 µg/ml), without affecting other Candida species, Aspergillus fumigatus, or HepG2 cells. Remarkably, it enhances the efficacy of fluconazole against azole-resistant C. albicans strains, showing a significant decrease in MICs (1 and 0.0078 µg/ml alone and in combination, respectively). PF-1163A distinguishes itself from PF-1163B by its more polar nature.

PF-1163A

PF-1163A

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Catalog No. TN7560Cas No. 258871-59-9
PF-1163A, a depsipeptide antifungal compound isolated from Penicillium, blocks ergosterol synthesis with an IC50 of 12 ng/ml. This compound specifically inhibits the enzyme ERG25p, a C-4 methyl oxidase in the ergosterol biosynthetic pathway, leading to its antifungal activity. Notably, in Saccharomyces cerevisiae modified to express ERG biosynthesis genes, PF-1163A exhibits an inhibition concentration (MIC value) of 12.5 µg/ml against ERG25p, though strains overexpressing ERG25p show resistance. Additionally, PF-1163A effectively suppresses the growth of Candida albicans (MIC = 8 µg/ml), without affecting other Candida species, Aspergillus fumigatus, or HepG2 cells. Remarkably, it enhances the efficacy of fluconazole against azole-resistant C. albicans strains, showing a significant decrease in MICs (1 and 0.0078 µg/ml alone and in combination, respectively). PF-1163A distinguishes itself from PF-1163B by its more polar nature.
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Description
PF-1163A, a depsipeptide antifungal compound isolated from Penicillium, blocks ergosterol synthesis with an IC50 of 12 ng/ml. This compound specifically inhibits the enzyme ERG25p, a C-4 methyl oxidase in the ergosterol biosynthetic pathway, leading to its antifungal activity. Notably, in Saccharomyces cerevisiae modified to express ERG biosynthesis genes, PF-1163A exhibits an inhibition concentration (MIC value) of 12.5 µg/ml against ERG25p, though strains overexpressing ERG25p show resistance. Additionally, PF-1163A effectively suppresses the growth of Candida albicans (MIC = 8 µg/ml), without affecting other Candida species, Aspergillus fumigatus, or HepG2 cells. Remarkably, it enhances the efficacy of fluconazole against azole-resistant C. albicans strains, showing a significant decrease in MICs (1 and 0.0078 µg/ml alone and in combination, respectively). PF-1163A distinguishes itself from PF-1163B by its more polar nature.
Chemical Properties
Molecular Weight477.6
FormulaC27H43NO6
Cas No.258871-59-9
SmilesC([C@H]1C(=O)O[C@H](C[C@H](CCC)O)CC[C@H](C)CCCCC(=O)N1C)C2=CC=C(OCCO)C=C2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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