| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Isoconazole nitrate targets fungal lanosterol 14α-demethylase, a cytochrome P450 enzyme involved in the biosynthesis of ergosterol, a key component of the fungal cell membrane. By inhibiting this enzyme, isoconazole blocks ergosterol synthesis, disrupting the fungal cell membrane and leading to fungal cell death. It also has antibacterial activity against Gram-positive bacteria.
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| ln Vitro |
Independent of its suppression of ergosterol synthesis, isoconazole nitrate also has a number of additional effects on fungal membranes. In vitro exposure to isoconazole nitrate (ISN) results in a sharp reduction in cellular adenosine triphosphate (ATP) within 10 minutes [1]. Through its effects on cell membrane formation and organization, isoconazole nitrate (1, 10 μg/mL) promotes a blockage of cell division in vitro. Fungal cells undergo necrosis and die when exposed to isoconazole nitrate (50, 100 μg/mL) [1].
In vitro, isoconazole nitrate has broad-spectrum antimicrobial activity. It is highly effective against a range of fungi, including dermatophytes, Candida species, and Malassezia. It also has activity against Gram-positive bacteria. Its rapid absorption and low systemic exposure have been characterized. |
| ln Vivo |
In vivo, isoconazole nitrate is used topically to treat fungal skin infections. Its rapid absorption and low systemic exposure make it suitable for topical application. It is effective in treating dermatophytosis, candidiasis, and pityriasis versicolor.
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| Enzyme Assay |
In vitro antimicrobial assays for isoconazole nitrate involve determining its minimum inhibitory concentration (MIC) against a panel of fungal and bacterial strains. Broth microdilution or agar dilution methods are used.
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| Cell Assay |
In vitro cell-based assays for isoconazole nitrate are not typically performed. Its antifungal activity is characterized by MIC determinations. Its effects on fungal cell membrane integrity can be assessed by microscopy.
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| Animal Protocol |
In vivo animal experiments for isoconazole nitrate have been conducted in models of fungal skin infections. Animals are infected with fungi and treated topically with the compound. Efficacy is measured by reduction in skin lesions and fungal burden.
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| ADME/Pharmacokinetics |
Isoconazole nitrate has a molecular weight of 479.14 and a molecular formula of C18H14Cl4N2O·HNO3. It is a white solid with a melting point of 178-186°C. It is typically stored at room temperature in a cool, dark place.
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| Toxicity/Toxicokinetics |
Isoconazole nitrate is a clinically used antifungal agent with a well-established safety profile. It is generally well-tolerated when applied topically. It may cause local skin irritation in some individuals. It is a prescription drug for clinical use under proper authorization.
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| References |
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| Additional Infomation |
Isoconazole nitrate is a synthetic imidazole antifungal agent. It is a broad-spectrum antimicrobial with antifungal and Gram-positive antibacterial activity. It is used to treat dermatophytosis, candidiasis, and pityriasis versicolor. It has rapid absorption and low systemic exposure.
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| Molecular Formula |
C18H15CL4N3O4
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|---|---|
| Molecular Weight |
479.1414
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| Exact Mass |
476.981
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| CAS # |
24168-96-5
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| Related CAS # |
27523-40-6;24168-96-5 (nitrate);
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| PubChem CID |
159968
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| Appearance |
White to off-white solid powder
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| Density |
1.4 g/cm3
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| Boiling Point |
555.1ºC at 760 mmHg
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| Melting Point |
178-182ºC
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| Flash Point |
289.5ºC
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| LogP |
6.63
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
431
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NNGQLSIGRSTLLU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14Cl4N2O.HNO3/c19-12-4-5-13(17(22)8-12)18(9-24-7-6-23-11-24)25-10-14-15(20)2-1-3-16(14)21;2-1(3)4/h1-8,11,18H,9-10H2;(H,2,3,4)
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| Chemical Name |
1-[2-(2,4-dichlorophenyl)-2-[(2,6-dichlorophenyl)methoxy]ethyl]imidazole;nitric acid
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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. |
| 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) |
DMSO : ~100 mg/mL (~208.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.22 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 25.0 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: ≥ 2.5 mg/mL (5.22 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 25.0 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: ≥ 2.5 mg/mL (5.22 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 | 2.0871 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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