Name: Ciclopirox ethanolamine
Brand: Selleck Chemicals
SKU: S3019
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

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

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COA
NMR
SDS
Datasheet

99.91

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel GluR
Other ATPase Inhibitors	(-)-Blebbistatin Thapsigargin Brefeldin A (BFA chemical) CB-5083 Bufalin Sodium orthovanadate Golgicide A Oleic Acid Saikosaponin D CDN1163

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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 1 40%PEG300 2 5%Tween80 3 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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	268.35	Formula	C₁₂H₁₇NO₂.C₂H₇NO	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	41621-49-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Ciclopirox olamine, HOE 296,Ciclopiroxolamine			Smiles	CC1=CC(=O)N(C(=C1)C2CCCCC2)O.C(CO)N

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
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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12760852/ [2] https://pubmed.ncbi.nlm.nih.gov/19307370/ [3] https://pubmed.ncbi.nlm.nih.gov/12760852/

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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Ciclopirox ethanolamine ATPase inhibitor

Chemical Structure

Molecular Weight: 268.35