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Ciclopirox ethanolamine ATPase inhibitor

Cat.No.S3019

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

Chemical Structure

Molecular Weight: 268.35

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 268.35 Formula

C12H17NO2.C2H7NO

 Storage (From the date of receipt)
CAS No. 41621-49-2 Download SDF Storage of Stock Solutions

Synonyms Ciclopirox olamine, HOE 296,Ciclopiroxolamine Smiles CC1=CC(=O)N(C(=C1)C2CCCCC2)O.C(CO)N

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (149.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Features
Exhibits antifungal activity via a specific iron limiation mechanism, with no single case of fungal resistance reported.
Targets/IC50/Ki
ATPase [3]
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

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