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Ciclopirox ethanolamine

Name: Ciclopirox ethanolamine
Brand: Selleck Chemicals
SKU: S3019
Rating: 5 (8 reviews)

Synonyms: Ciclopirox olamine, HOE 296,Ciclopiroxolamine

Catalog No.S3019 Purity: 99.91%

Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296,Ciclopiroxolamine) is a broad-spectrum antifungal agent working as an iron chelator.

Ciclopirox ethanolamine Chemical Structure

CAS: 41621-49-2

Selleck's Ciclopirox ethanolamine has been cited by 8 publications

Purity & Quality Control

Batch: S301901 DMSO] 40 mg/mL] false] Ethanol] 30 mg/mL] false] Water] Insoluble] false Purity: 99.91%

99.91

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Biological Activity

Description

Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296,Ciclopiroxolamine) is a broad-spectrum antifungal agent working as an iron chelator.

Features

Exhibits antifungal activity via a specific iron limiation mechanism, with no single case of fungal resistance reported.

Targets

ATPase ^[3]

In vitro
In vitro	Ciclopirox significantly inhibits the growth of C. albicans strain SC5314 cells, with MIC₈₀s of 1.0-2.0 μg/mL, growth decreased dramatically at the concentrations of >0.6 μg/mL, and almost complete growth inhibition at concentration of 0.7 μg/mL, unlike fluconazole which shows a much wider range of concentrations with intermediate inhibition. Like iron chelator bipyridine, Ciclopirox reduces cell growth by binding to iron ions, which can be reversed by addition of FeCl₃. Moreover, Ciclopirox treatment at subinhibitory concentration (0.6 μg/mL) only moderately reduces the virulence genes such as genes encoding secreted proteinases or lipases, but leads to a distinct up- or down-regulation of genes encoding iron permeases or transporters (FTR1, FTR2, and FTH1), a copper permease (CCC2), an iron reductase (CFL1), and a siderophore transporter (SIT1). Although the Candida drug resistance genes CDR1 and CDR2 are up-regulated after Ciclopirox treatment, no change in resistance or increased tolerance could be observed even after an incubation period of 6 months, in contrast to fluconazole in which the MICs for cells noticeably increase after 2 months. ^[1] Ciclopirox inhibits the growth of Aspergillus fumigatus strain B5233 with IC50 of 4.22 μM, more potently compared with deferiprone with IC50 of 1.29 mM. ^[2]
Cell Research	Cell lines	C. albicans strain SC5314
	Concentrations	Dissolved in DMSO, final concentrations 10 μg/mL
	Incubation Time	1-10 hours
	Method	Sabouraud glucose medium (2%) is used for cell culture growth, and RPMI 2% glucose medium and 2% Sabouraud glucose medium are used for MIC determinations. For cell culture growth curves, 220 mL of 2% Sabouraud glucose medium containing different concentrations of Ciclopirox are inoculated with 10⁵ cells/mL, and the mixture is shaken at 160 rpm and 37 °C for 1-10 hours. Growth is measured photometrically at 630 nm. FeCl₃ or 2,2'-bipyridine is added to the medium at different concentrations for inhibition studie

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00990587	Completed	Hematologic Malignancy\|Acute Lymphocytic Leukemia\|Chronic Lymphocytic Leukemia\|Myelodysplasia\|Acute Myeloid Leukemia\|Chronic Myelogenous Leukemia\|Hodgkin''s Disease	University Health Network Toronto\|The Leukemia and Lymphoma Society	October 2009	Phase 1
NCT01646580	Terminated	Dermatomycoses	Ferrer Internacional S.A.	October 2008	Phase 4

References

Chemical lnformation & Solubility

Molecular Weight	268.35	Formula	C₁₂H₁₇NO₂.C₂H₇NO
CAS No.	41621-49-2	SDF	Download Ciclopirox ethanolamine SDF
Smiles	CC1=CC(=O)N(C(=C1)C2CCCCC2)O.C(CO)N
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 40 mg/mL ( (149.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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