| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Democonazole targets the fungal enzyme CYP450 14α-lanosterol demethylase (also known as sterol 14α-demethylase), which catalyzes a key step in the ergosterol biosynthesis pathway. By inhibiting this enzyme, democonazole blocks the conversion of lanosterol to ergosterol, leading to the accumulation of toxic sterol intermediates and depletion of ergosterol in the fungal cell membrane. Ergosterol depletion disrupts membrane integrity and fluidity, impairing membrane-bound enzyme function and increasing membrane permeability. The resulting loss of membrane function leads to growth inhibition and ultimately cell death. Democonazole's lipophilic properties facilitate its penetration through the fungal cell wall and membrane to reach its target enzyme.
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| ln Vitro |
In vitro, democonazole demonstrates antifungal activity against a range of fungal pathogens. The compound's activity is typically assessed by determining the minimum inhibitory concentration (MIC) against various fungal strains using broth microdilution or agar dilution methods. Democonazole inhibits fungal growth by blocking ergosterol synthesis, which is essential for fungal cell membrane integrity. The compound shows activity against dermatophytes, yeasts, and other clinically relevant fungi. The lipophilic nature of democonazole contributes to its ability to penetrate fungal cells and reach its intracellular target.
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| ln Vivo |
In vivo efficacy data for democonazole is limited in the available literature. As an antimycotic agent, democonazole is expected to be effective in treating fungal infections in vivo, consistent with the mechanism of action of other ergosterol biosynthesis inhibitors. The compound's lipophilic properties likely contribute to good tissue distribution and penetration into fungal infection sites. However, specific in vivo studies and clinical data for democonazole are not extensively reported in the available literature. Democonazole is primarily used as a research tool for studying antifungal mechanisms.
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| Enzyme Assay |
Democonazole's enzyme inhibition is evaluated using biochemical assays with the target enzyme CYP450 14α-lanosterol demethylase. In these assays, the enzyme is incubated with the substrate lanosterol and varying concentrations of democonazole; the production of the demethylated product is measured by HPLC or mass spectrometry. IC50 values are calculated from dose-response curves. These assays provide quantitative information on the potency of democonazole as an inhibitor of ergosterol biosynthesis.
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| Cell Assay |
Democonazole is tested on cultured fungal cells (e.g., Candida albicans, Aspergillus fumigatus, Trichophyton species). Fungal cells are treated with varying concentrations of democonazole; growth inhibition is measured by optical density, colony counting, or metabolic activity assays (e.g., XTT reduction). Ergosterol content in treated cells is measured by HPLC or spectrophotometric methods to confirm target engagement. Membrane integrity is assessed using fluorescent dyes or by measuring leakage of intracellular contents. These cell-based assays provide evidence for the antifungal activity and mechanism of action of democonazole.
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| Animal Protocol |
Democonazole is evaluated in animal models of fungal infection. In these studies, animals (typically mice or rats) are infected with a pathogenic fungus (e.g., Candida albicans) and treated with democonazole at various doses. Efficacy is assessed by measuring fungal burden in target organs (e.g., kidney, liver), survival, and clinical signs of infection. Pharmacokinetic-pharmacodynamic relationships are established to guide dose selection. These in vivo studies are essential for demonstrating the therapeutic potential of democonazole.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for democonazole is limited in the available literature. As a lipophilic compound, democonazole is expected to be well-absorbed following oral administration and to distribute extensively into tissues. The compound is likely metabolized in the liver by cytochrome P450 enzymes and excreted in bile and urine. However, specific pharmacokinetic parameters such as half-life, volume of distribution, and clearance have not been extensively reported.
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| Toxicity/Toxicokinetics |
The toxicity profile of democonazole is not extensively characterized in the available literature. As an ergosterol biosynthesis inhibitor targeting fungal CYP450 enzymes, democonazole is expected to have selective toxicity for fungal cells over mammalian cells, as mammals use cholesterol rather than ergosterol in their cell membranes. However, potential off-target effects on mammalian CYP450 enzymes may contribute to drug-drug interactions and toxicity. Comprehensive toxicological studies have not been reported in the available literature.
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| References |
:Arzneimittelforschung. 1986 Oct;36(10):1440-1.
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| Additional Infomation |
Democonazole is an antimycotic agent used primarily in research settings. The compound is not approved as a therapeutic agent by any regulatory authority. It is used as a research tool for studying the ergosterol biosynthesis pathway and for developing new antifungal therapies. Democonazole belongs to the class of azole antifungals, which are widely used clinically for the treatment of fungal infections. The compound's mechanism of action—inhibition of CYP450 14α-lanosterol demethylase—is shared with clinically used azole antifungals such as fluconazole and itraconazole. Research on democonazole contributes to the understanding of antifungal drug development and resistance mechanisms.
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| Molecular Formula |
C19H15CL3N2O2
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|---|---|
| Molecular Weight |
409.6936
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| Exact Mass |
408.02
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| Elemental Analysis |
C, 55.70; H, 3.69; Cl, 25.96; N, 6.84; O, 7.81
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| CAS # |
70161-09-0
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| PubChem CID |
3033986
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| Appearance |
oily liquid
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| Density |
1.32g/cm3
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| Boiling Point |
569.8ºC at 760 mmHg
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| Flash Point |
298.4ºC
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| Index of Refraction |
1.601
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| LogP |
5.894
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
458
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1OCCO/C(=C/N2C=CN=C2)/C3=C(C=C(C=C3)Cl)Cl)Cl
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| InChi Key |
ABVFVJRTKMVJMV-XDHOZWIPSA-N
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| InChi Code |
InChI=1S/C19H15Cl3N2O2/c20-14-1-4-16(5-2-14)25-9-10-26-19(12-24-8-7-23-13-24)17-6-3-15(21)11-18(17)22/h1-8,11-13H,9-10H2/b19-12+
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| Chemical Name |
1-[(E)-2-[2-(4-chlorophenoxy)ethoxy]-2-(2,4-dichlorophenyl)ethenyl]imidazole
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| Synonyms |
Democonazole
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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 | 2.4409 mL | 12.2043 mL | 24.4087 mL | |
| 5 mM | 0.4882 mL | 2.4409 mL | 4.8817 mL | |
| 10 mM | 0.2441 mL | 1.2204 mL | 2.4409 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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