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| 1g |
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Purity: ≥98%
| Targets |
Miconazole Nitrate targets the fungal enzyme lanosterol 14α-demethylase (CYP51), which is involved in the biosynthesis of ergosterol. By inhibiting this enzyme, it prevents the conversion of lanosterol to ergosterol, leading to the accumulation of toxic 14α-methyl sterols and depletion of ergosterol. This disrupts the fungal cell membrane, inhibiting fungal growth and leading to cell death. Miconazole has broad-spectrum activity against dermatophytes, yeasts, and other fungi.
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| ln Vitro |
In vitro, Miconazole Nitrate demonstrates potent antifungal activity against a wide range of fungal pathogens, including Candida species, dermatophytes, and Malassezia. It inhibits fungal growth in a concentration-dependent manner. The compound's activity is measured by determining the minimum inhibitory concentration (MIC) against various fungal strains. Miconazole is effective against both yeast and mold forms of fungi.
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| ln Vivo |
In vivo, Miconazole Nitrate is used topically for the treatment of skin and mucosal fungal infections. It is effective against tinea infections (ringworm), candidiasis (thrush), and pityriasis versicolor. It is applied to the affected area once or twice daily for 2-4 weeks. The compound provides symptomatic relief and eliminates the fungal infection. It is not significantly absorbed through the skin, minimizing systemic side effects.
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| Enzyme Assay |
In vitro antifungal susceptibility assays for Miconazole Nitrate are performed using standard broth microdilution or agar diffusion methods. Various fungal strains are cultured in appropriate media and exposed to varying concentrations of Miconazole Nitrate. The minimum inhibitory concentration (MIC) is determined after incubation at 35-37°C for 24-48 hours. The compound's activity is compared to standard antifungal agents for quality control.
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| Cell Assay |
In vitro cell-based assays for Miconazole Nitrate are performed using mammalian cell lines (e.g., keratinocytes or fibroblasts) to assess cytotoxicity. Cells are cultured in appropriate media and treated with Miconazole Nitrate at various concentrations. Cell viability is measured by MTT or neutral red uptake assays. The compound's selectivity index is calculated by comparing its cytotoxic concentration to its antifungal concentration.
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| Animal Protocol |
In vivo animal studies for Miconazole Nitrate are conducted in models of fungal infection. Animals are infected with a fungal pathogen (e.g., Candida albicans) and treated with Miconazole Nitrate topically or systemically. The reduction in fungal burden is assessed by colony counting from infected tissues. Efficacy is compared to untreated controls and standard antifungal agents.
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| ADME/Pharmacokinetics |
Miconazole Nitrate is minimally absorbed through the skin and mucous membranes. When applied topically, systemic absorption is low, and the compound remains primarily at the site of application. It is metabolized in the liver and excreted in feces and urine. The compound's pharmacokinetic profile supports its use as a topical antifungal agent.
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| Toxicity/Toxicokinetics |
Miconazole Nitrate is generally well-tolerated when used topically. Local side effects may include irritation, burning, or itching at the application site. Systemic toxicity is rare due to minimal absorption. It is contraindicated in patients with known hypersensitivity to miconazole or other imidazole antifungals. It is not for systemic use.
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| References | |
| Additional Infomation |
Miconazole Nitrate is a broad-spectrum antifungal agent used for the treatment of various fungal infections. It inhibits ergosterol synthesis by targeting lanosterol 14α-demethylase. Miconazole is effective against dermatophytes, yeasts, and other fungi. It is available in topical formulations for skin and mucosal infections. This product is for research and topical use.
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| Molecular Formula |
C18H14N2OCL4.HNO3
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|---|---|
| Molecular Weight |
479.1414
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| CAS # |
228321-87-7
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| Related CAS # |
22916-47-8 (free); 22832-87-7 (nitrate)
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| Appearance |
White to off-white solid powder
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| Melting Point |
178-184 °C
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| SMILES |
[N+]([O-])(O)=O.ClC1C=C(Cl)C=CC=1COC(C1C=CC(Cl)=CC=1Cl)CN1C=CN=C1
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| InChi Key |
BYBLEWFAAKGYCD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14Cl4N2O/c19-13-2-1-12(16(21)7-13)10-25-18(9-24-6-5-23-11-24)15-4-3-14(20)8-17(15)22/h1-8,11,18H,9-10H2
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| Chemical Name |
1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole
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| Synonyms |
R-18134; R 18134; R18134Desenex, Monistat, Zeasorb-AF, Brentan, Dactarin, R-14,889
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0871 mL | 10.4354 mL | 20.8707 mL | |
| 5 mM | 0.4174 mL | 2.0871 mL | 4.1741 mL | |
| 10 mM | 0.2087 mL | 1.0435 mL | 2.0871 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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