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Ciclopirox ethanolamine

Cat. No. M3593
Ciclopirox ethanolamine Structure
Size Price Availability Quantity
1g USD 160 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ciclopirox ethanolamine is a broad-spectrum antifungal agent working as an iron chelator. Ciclopirox inhibits nearly all clinically relevant dermatophytes, yeasts, and molds, including the frequently azole-resistant Candida species Candida glabrata, Candida krusei, and Candida guilliermondii. In addition, Ciclopirox acts against a wide range of bacteria including many gram-positive and gram-negative species pathogenic for humans. Ciclopirox inhibits dermatophytes and yeasts pathogenic with MICs of 0.98-3.9 μg/mL. Ciclopirox can be rapidly taken up by growing C. albicans cells, and intracellular accumulation of Ciclopirox can lead to levels 200 times greater than those in the medium. More than 97% of the accumulated Ciclopirox is bound largely irreversibly to different cell structures and organelles such as the cell membrane, cell wall, mitochondria, microsomes, and ribosomes, while only small amounts are found in the cytosolic fraction. Moreover, Ciclopirox is neither metabolized nor degraded. In addition, Ciclopirox at higher concentrations leads to cellular leakage, causing the loss of folin-positive substances and potassium ions from the cell without affecting the fungal cell wall. Ciclopirox inhibits the synthesis of protein, RNA, and DNA in growing fungal cells, possibly by blocking the uptake of precursors of the macromolecules or by blocking the uptake of essential ions such as potassium ions and phosphates. Similar to rilopirox, Ciclopirox at subinhibitory concentration causes modifications in particle distribution within the plasma membrane, having an effect on the adherence of C. albicans to buccal and vaginal epithelial cells. The chelation of metal ions and the inhibition of iron-dependent enzymes play a primary role in the action of Ciclopirox.Ciclopirox alone potently inhibits the growth of Aspergillus fumigatus B5233 conidia, and Ciclopirox in combination with ketoconazole displays synergistic antifungal activity.

Protocol
Cell Experiment
Cell lines C. albicans strain SC5314
Preparation method Using sabouraud glucose medium (2%) for cell culture growth, and RPMI 2% glucose medium and 2% Sabouraud glucose medium are used for MIC determinations. For cell culture growth curves, inoculating 220 mL of 2% Sabouraud glucose medium which contains different concentrations of Ciclopirox with 105 cells/mL, and shaking the mixture at 160 rpm and 37 °C for 1-10 hours. Measuring growth photometrically at 630 nm. Adding feCl3 or 2,2'-bipyridine to the medium at different concentrations for inhibition studie
Concentrations Dissolved in DMSO, final concentrations 10 μg/mL
Incubation time 1-10 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 268.35
Formula C12H17NO2.C2H7NO
CAS Number 41621-49-2
Purity >99%
Solubility Ethanol 30 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




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