Ciclopirox ATPase inhibitor

Ciclopirox (HOE 296b, Penlac) is a broad-spectrum antifungal agent working as an iron chelator. This compound is a broad-spectrum antifungal agent working as an iron chelator. This chemical is a broad-spectrum antifungal agent working as an iron chelator.

Ciclopirox  ATPase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 207.27

Purity & Quality Control

Batch: S252801 DMSO]41 mg/mL]false]Ethanol]41 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Related Products

Signaling Pathway

Mechanism of Action

Targets
ATPase [6]

In vitro

In vitro

Ciclopirox olamine (CPX) is a lipophilic bidentate iron chelator that stabilizes HIF-1alpha under normoxic conditions at lower concentrations than other iron chelators, probably by inhibiting HIF-1alpha hydroxylation. This compound-induced HIF-1 mediates reporter gene activity and endogenous HIF-1 target gene expression, including elevation of transcription, mRNA, and protein levels of the vascular endothelial growth factor (VEGF).[1] It inhibits growth of C. albicans yeast and hyphal cells in a dose-dependent manner. [2] This chemical blocks H2O2-induced mitochondrial injury by maintaining mitochondrial transmembrane potential (Deltapsim). It completely blocks H2O2-stimulated release of lactate dehydrogenase (a marker of cell death) and decreases in MTT reduction (a marker of mitochondrial function) in adenocarcinoma SK-HEP-1 cells. This compound effectively inhibits H2O2-induced mitochondrial permeability transition pore (MPTP) opening. [3] It increases the MTP, maintained it high, and blocks the ATP depletion in glucose-deprived SIN-1-treated astrocytes. This chemical protects astrocytes from peroxynitritecytotoxicity by attenuating peroxynitrite-induced mitochondrial dysfunction. [4] It is a substituted pyridone antimycotic drug, unrelated to the imidazole derivatives and its topical application ensures maximum local bioavailability. This compound acts on fungi by inhibiting the intracellular uptake of essential substrates and ions and this probably acts on the Candida ability to express its adherence mechanisms. [5]

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

References

  • https://pubmed.ncbi.nlm.nih.gov/12594177/
  • https://pubmed.ncbi.nlm.nih.gov/15790671/
  • https://pubmed.ncbi.nlm.nih.gov/15806112/
  • https://pubmed.ncbi.nlm.nih.gov/12243770/
  • https://pubmed.ncbi.nlm.nih.gov/1492854/

Chemical Information

Molecular Weight 207.27 Formula

C12H17NO2

CAS No. 29342-05-0 SDF Download SDF
Synonyms HOE 296b, Penlac
Smiles CC1=CC(=O)N(C(=C1)C2CCCCC2)O

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 41 mg/mL ( (197.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 41 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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