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| 250mg |
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| 1g |
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Purity: ≥98%
Ciclopirox ethanolamine (formerly HOE-296; HOE296; Ciclopirox olamine), the ethanolamine salt of Ciclopirox, is a novel, investigational, synthetic, potent and broad-spectrum antifungal agent working as an iron chelator and used as an antifungal agent for topical dermatologic treatment of superficial mycoses. It is currently being investigated as an alternative treatment to ketoconazole for seborrhoeic dermatitis as it suppresses growth of the yeast Malassezia furfur.It acts by inhibiting the membrane transfer system by interrupting the Na+ K+ ATPase. Ciclopirox ethanolamine suppresses many clinically relevant dermatophytes, yeasts, and molds, including the frequently azole-resistant Candida species Candida glabrata, and Candida guilliermondii. Moreover, Ciclopirox has been proved to inhibit a wide range of bacteria in humans, including many gram(+) and gram (-) species pathogenic bacteria.
| ln Vitro |
In a study to further explain the mechanism of Ciclopirox GMP, many S. cerevisiae mutants were examined and tested. Interpretation of the effects of pharmacological treatments and mutations suggests that Ciclopirox GMP may act by altering some aspects of DNA repair, cell division signaling and structure (mitotic spindle), and intracellular transport [2]. Ciclopirox GMP is a broad-spectrum antifungal drug with anti-inflammatory characteristics that is effective against the yeast Malassezia spp, which is associated with seborrheic dermatitis [3]. Ciclopirox (olamine) (0.9 μM, 24 h) protects human iPSC-derived RPE cells subjected to TBHP-induced oxidative damage [2].
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| ln Vivo |
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: iPSC-derived RPE cells Tested Concentrations: 0.9 μM Incubation Duration: 24 h Experimental Results: Protected human iPSC-derived RPE cells exposed to TBHP-induced cell death. Real Time qPCR[2] Cell Types: iPSC -derived RPE cells Tested Concentrations: 0.9 μM Incubation Duration: 24 h Experimental Results: Expressed RPE markers (RPE65, BEST1, MITF). |
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| Animal Protocol |
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| References |
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| Additional Infomation |
Ciclopirox Olamine is the olamine salt form of ciclopirox, a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. Ciclopirox exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).
A cyclohexane and pyridinone derivative that is used for the treatment of fungal infections of the skin and nails, and for treatment of VAGINAL YEAST INFECTIONS. See also: Monoethanolamine (has part); Ciclopirox (has active moiety); Ciclopirox olamine; salicylic acid (component of) ... View More ... |
| Molecular Formula |
C12H17NO2.C2H7NO
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| Molecular Weight |
268.35
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| Exact Mass |
268.178
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| CAS # |
41621-49-2
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| Related CAS # |
Ciclopirox;29342-05-0;Ciclopirox olamine;41621-49-2
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| PubChem CID |
38911
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| Appearance |
White to yellow solid powder
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| Boiling Point |
350ºC at 760 mmHg
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| Melting Point |
144ºC
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| Flash Point |
165.5ºC
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| LogP |
2.079
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
335
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C=C(C)C=C(C2CCCCC2)N1O.NCCO
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| InChi Key |
HKUKJIQHPXYJTP-UHFFFAOYSA-O
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| InChi Code |
InChI=1S/C12H16NO2.C2H7NO/c1-9-7-11(13(15)12(14)8-9)10-5-3-2-4-6-10;3-1-2-4/h7-8,10H,2-6H2,1H3;4H,1-3H2/q-1;/p+1
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| Chemical Name |
6-Cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone Ethanolamine Salt
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (7.75 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7265 mL | 18.6324 mL | 37.2648 mL | |
| 5 mM | 0.7453 mL | 3.7265 mL | 7.4530 mL | |
| 10 mM | 0.3726 mL | 1.8632 mL | 3.7265 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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