Ciclopirox ethanolamine

Catalog No.S3019 Batch:S301901

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Technical Data

Formula

C12H17NO2.C2H7NO
Molecular Weight 268.35 CAS No. 41621-49-2
Solubility (25°C)* In vitro DMSO 40 mg/mL (149.05 mM)
Ethanol 30 mg/mL (111.79 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.000mg/ml (7.45mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296,Ciclopiroxolamine) is a broad-spectrum Fungal agent working as an iron chelator.
Targets
ATPase
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 Transmembrane Transporters (FTR1, FTR2, and FTH1), a copper permease (CCC2), an iron reductase (CFL1), and a siderophore Transmembrane 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. 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.

Features Exhibits Fungal activity via a specific iron limitation mechanism, with no single case of Fungal resistance reported.

Protocol (from reference)

Cell Assay:

[1]
  • 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

References

  • https://pubmed.ncbi.nlm.nih.gov/12760852/
  • https://pubmed.ncbi.nlm.nih.gov/19307370/
  • https://pubmed.ncbi.nlm.nih.gov/12760852/

Sellecks Ciclopirox ethanolamine Has Been Cited by 8 Publications

Inference of glioblastoma migration and proliferation rates using single time-point images [ Commun Biol, 2023, 6(1):402] PubMed: 37055469
Iron-dependent epigenetic modulation promotes pathogenic T cell differentiation in lupus [ J Clin Invest, 2022, 132(9)e152345] PubMed: 35499082
TRIM7 modulates NCOA4-mediated ferritinophagy and ferroptosis in glioblastoma cells [ Redox Biol, 2022, 56:102451] PubMed: 36067704
Leveraging patient derived models of FGFR2 fusion positive intrahepatic cholangiocarcinoma to identify synergistic therapies [ NPJ Precis Oncol, 2022, 6(1):75] PubMed: 36274097
MicroRNA-4735-3p Facilitates Ferroptosis in Clear Cell Renal Cell Carcinoma by Targeting SLC40A1 [ Anal Cell Pathol (Amst), 2022, 2022:4213401] PubMed: 35646516
Transcriptional Repression of Ferritin Light Chain Increases Ferroptosis Sensitivity in Lung Adenocarcinoma [ Front Cell Dev Biol, 2021, 9:719187] PubMed: 34765600
Synthetic Derivatives of Ciclopirox are Effective Inhibitors of Cryptococcus neoformans [ ACS Omega, 2021, 6(12):8477-8487] PubMed: 33817509
High-throughput functional annotation of natural products by integrated activity profiling [ bioRxiv, 2019, 10.1101/748129] PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.