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Eberconazole Nitrate

Alias: EberconazolEberconazole Nitrate Ebernet Eberconazolum
Cat No.:V20364 Purity: ≥98%
Eberconazole nitrate is a dicloimidazole analogue with antifungal activity.
Eberconazole Nitrate
Eberconazole Nitrate Chemical Structure CAS No.: 130104-32-4
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Eberconazole Nitrate:

  • Eberconazole
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Eberconazole nitrate is a dicloimidazole analogue with antifungal activity. Eberconazole nitrate is more effective than Clotrimazole, Ketoconazole and Miconazole. Eberconazole nitrate may be used for studying dermatophytosis via topical administration.
Eberconazole Nitrate (CAS 130104-32-4) is an azole antifungal agent and a broad-spectrum imidazole derivative. It is a dicloimidazole analogue. Eberconazole nitrate is more effective than clotrimazole, ketoconazole, and miconazole. It may be used for studying dermatophytosis via topical administration. The compound is a dichloro imidazole analogue with antifungal activity.
Biological Activity I Assay Protocols (From Reference)
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

[1]. In vitro activities of the new antifungal drug eberconazole and three other topical agents against 200 strains of dermatophytes. J Clin Microbiol. 2003;41(11):5209-5211.

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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
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 Data
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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