| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Eberconazole nitrate targets fungal sterol 14α-demethylase (CYP51), an enzyme involved in the biosynthesis of ergosterol, a key component of fungal cell membranes. As an azole antifungal, it inhibits CYP51, leading to depletion of ergosterol and accumulation of toxic sterol intermediates. This disrupts fungal cell membrane integrity and function, resulting in fungal growth inhibition and cell death.
|
|---|---|
| ln Vitro |
In vitro, eberconazole nitrate shows broad-spectrum antifungal activity. It is more effective than clotrimazole, ketoconazole, and miconazole. The compound's antifungal activity has been demonstrated against various dermatophytes and other fungal pathogens. Its potency has been characterized in minimum inhibitory concentration (MIC) assays. The compound is a dicloimidazole analogue.
|
| ln Vivo |
In vivo, eberconazole nitrate may be used for studying dermatophytosis via topical administration. Its antifungal efficacy has been demonstrated in animal models of fungal skin infections. The compound's topical application allows for direct delivery to the site of infection, minimizing systemic exposure and potential side effects. Further clinical studies would be needed for therapeutic approval.
|
| Enzyme Assay |
In vitro antifungal susceptibility assays for eberconazole nitrate follow CLSI or EUCAST guidelines. Fungal cultures (e.g., dermatophytes, Candida species) are grown in appropriate media. Various concentrations of eberconazole nitrate are added. Minimum inhibitory concentration (MIC) is determined by broth microdilution or agar dilution methods. Fungal growth is assessed by optical density or visual inspection.
|
| Cell Assay |
For in vitro cellular assays, fungal cells are cultured and treated with various concentrations of eberconazole nitrate. Fungal viability is assessed by measuring metabolic activity (e.g., XTT reduction assay) or by colony-forming unit (CFU) counting. Ergosterol content may be measured by HPLC to confirm the mechanism of action. Cytotoxicity against mammalian cells is assessed using MTT assays.
|
| Animal Protocol |
In vivo animal studies for eberconazole nitrate utilize models of dermatophytosis, such as guinea pig or mouse models of skin infection. The compound is applied topically at various concentrations. Infection severity is assessed by clinical scoring, fungal culture, and histopathological examination. Efficacy is compared to vehicle and reference antifungal agents (e.g., clotrimazole, ketoconazole).
|
| ADME/Pharmacokinetics |
Eberconazole nitrate has molecular weight of 392.24 g/mol and molecular formula C18H15Cl2N3O3. It is a nitrate salt. Purity is ≥98%. It is typically stored at room temperature. It is soluble in organic solvents. Pharmacokinetic properties after topical application include minimal systemic absorption. The compound is primarily used for topical antifungal research.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity of eberconazole nitrate has been evaluated in standard toxicology studies. As a topical antifungal, systemic toxicity is minimal due to limited absorption. Local skin irritation may occur. No significant systemic toxicity has been reported at therapeutic doses. The compound is for research use only and is not approved for human therapeutic use in most regions.
|
| References | |
| Additional Infomation |
Eberconazole Nitrate is an azole antifungal agent and broad-spectrum imidazole derivative. It is a dicloimidazole analogue. It is more effective than clotrimazole, ketoconazole, and miconazole. It may be used for studying dermatophytosis via topical administration. It is available for research purposes only.
|
| Molecular Formula |
C18H15CL2N3O3
|
|---|---|
| Molecular Weight |
392.236
|
| Exact Mass |
391.049
|
| CAS # |
130104-32-4
|
| Related CAS # |
Eberconazole;128326-82-9
|
| PubChem CID |
179851
|
| Appearance |
White to light yellow solid powder
|
| Boiling Point |
495ºC at 760 mmHg
|
| Flash Point |
253.2ºC
|
| Vapour Pressure |
1.86E-09mmHg at 25°C
|
| LogP |
5.101
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
26
|
| Complexity |
416
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
DPHMSVRBAXJSPF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H14Cl2N2.HNO3/c19-14-9-13-6-5-12-3-1-2-4-15(12)18(17(13)16(20)10-14)22-8-7-21-11-222-1(3)4/h1-4,7-11,18H,5-6H2(H,2,3,4)
|
| Chemical Name |
1-(2,4-dichloro-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl)-1H-imidazole nitrate
|
| Synonyms |
EberconazolEberconazole Nitrate Ebernet Eberconazolum
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~637.36 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.30 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 (5.30 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 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) 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 | 2.5495 mL | 12.7473 mL | 25.4946 mL | |
| 5 mM | 0.5099 mL | 2.5495 mL | 5.0989 mL | |
| 10 mM | 0.2549 mL | 1.2747 mL | 2.5495 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.