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| Targets |
The primary target of Oxiconazole nitrate is the fungal enzyme lanosterol 14α-demethylase (CYP51), which is involved in ergosterol biosynthesis. By inhibiting this enzyme, oxiconazole prevents the synthesis of ergosterol, a key component of the fungal cell membrane. This leads to membrane destabilization and fungal cell death. The compound also has antibacterial activity against some Gram-positive bacteria.
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| ln Vitro |
Oxyconazole (24 hours; 0-40 μM) suppresses the development of CRC cells [3]. Trichophyton, Aspergillus, and Candida are susceptible to the antifungal effects of oxyconazole [1]. Oxyconazole's antifungal activity [1]. Candida albicans Candida pneumonia Porphyromonas fumigatus Aspergillus flavus Mentagrophytes Trichophyton Rubrum Trichophyton oxyconazole A 0.03 μg/mL, a 0.01 μg/mL, and a 0.008 μg/mL, two μg/mL, two μg/mL, and two μg/mL
In vitro, oxiconazole nitrate has been shown to have antifungal activity against a range of dermatophytes and yeasts. It is effective against Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Malassezia furfur. In vitro susceptibility testing, such as broth microdilution, is used to determine the minimum inhibitory concentration (MIC) for various fungal isolates. |
| ln Vivo |
For 12 days, oxyconazole (50 mg/kg/day; IP) dramatically reduces the development of colorectal cancer cells [3].
In vivo, oxiconazole nitrate is effective in treating fungal skin infections. It is applied topically once or twice daily for 2-4 weeks, depending on the condition. The compound is well-tolerated and has low systemic absorption. It provides symptomatic relief and eradication of the fungal infection. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for oxiconazole nitrate involve measuring its inhibition of lanosterol 14α-demethylase (CYP51) activity. The assay uses a purified fungal CYP51 enzyme and a substrate, such as lanosterol. The production of ergosterol is measured using chromatographic methods. The compound is incubated with the enzyme and substrate at varying concentrations, and the IC50 is determined.
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| Cell Assay |
Cell Proliferation Assay[3]
Cell Types: HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 Tested Concentrations: 0-40 μM Incubation Duration: 24 hrs (hours) Experimental Results: For HCT116, SW480, RKO, DLD -1, SW620, LoVo and NCM460 demonstrated inhibitory activity IC50 of 25.86 μM, 27.34 μM, 21.01 μM, 25.56 μM, 21.75 μM, 24.87 μM and 126.4 μM. In vitro cell-based assays for oxiconazole nitrate are performed using fungal cultures. The fungus is grown in the presence of the compound, and the minimum inhibitory concentration (MIC) is determined. Time-kill studies can also be performed to assess the fungicidal activity. These assays confirm the compound's antifungal activity. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice (subcutaneous injection of HCT116 cells (1×107/mouse) [3]
Doses: 50 mg/kg/day Route of Administration: IP; 12 days. Experimental Results: Dramatically inhibited CRC cell growth, and No obvious side effects. In vivo animal experiments for oxiconazole nitrate are conducted using animal models of fungal skin infection, such as guinea pig models of dermatophytosis. The compound is applied topically, and its efficacy is evaluated by measuring the reduction in fungal load and the improvement in skin lesions. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of oxiconazole nitrate indicate that it is minimally absorbed through the skin after topical application. The compound has a molecular weight of 429.13 and a molecular formula of C18H15Cl4N3O·HNO3. It is a solid at room temperature. The compound is metabolized in the liver and excreted renally. Systemic exposure is low due to minimal absorption.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for oxiconazole nitrate indicate that it is generally well-tolerated when used topically. Common side effects include skin irritation, redness, and itching at the application site. The compound should be used with caution in patients with a history of hypersensitivity to imidazole antifungals.
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| References |
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| Additional Infomation |
Oxiconazole nitrate is an organic nitrate produced by the reaction of equimolar amounts of oxiconazole and nitric acid. It is an antifungal agent used in creams and powders to treat fungal skin infections. It has anti-infective activity. It is an organic nitrate belonging to the oxiconazole and imidazole classes of antifungal drugs. It contains an oxiconazole (1+) ligand. Oxiconazole nitrate is the nitrate form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Although its exact mechanism of action is not fully elucidated, like other azole antifungal drugs, oxiconazole likely inhibits cytochrome P450-dependent lanosterol demethylation. This prevents the synthesis of ergosterol, a key component of fungal cell membranes. By disrupting the synthesis and integrity of fungal cell membranes, oxiconazole alters the permeability of fungal cell membranes, promoting the loss of essential intracellular components and ultimately inhibiting fungal cell growth. See also: Oxiconazole (with active moiety).
Other information: Oxiconazole nitrate is a topical antifungal agent used for the treatment of fungal skin infections. It is also known as Oxiconazole. The compound is available as a cream, lotion, and powder. Its CAS number is 64211-46-7. |
| Molecular Formula |
C18H13CL4N3O.HNO3
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|---|---|
| Molecular Weight |
492.14
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| Exact Mass |
491.973
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| CAS # |
64211-46-7
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| Related CAS # |
Oxiconazole;64211-45-6
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| PubChem CID |
9556529
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| Appearance |
White to off-white solid powder
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| Boiling Point |
576.8ºC
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| Melting Point |
137-1380C
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| Flash Point |
302.6ºC
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| LogP |
6.155
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
506
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=C(C=C1Cl)Cl)CO/N=C(\CN2C=CN=C2)/C3=C(C=C(C=C3)Cl)Cl.[N+](=O)(O)[O-]
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| InChi Key |
WVNOAGNOIPTWPT-NDUABGMUSA-N
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| InChi Code |
InChI=1S/C18H13Cl4N3O.HNO3/c19-13-2-1-12(16(21)7-13)10-26-24-18(9-25-6-5-23-11-25)15-4-3-14(20)8-17(15)22;2-1(3)4/h1-8,11H,9-10H2;(H,2,3,4)/b24-18+;
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| Chemical Name |
(Z)-1-(2,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methoxy]-2-imidazol-1-ylethanimine;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 (~203.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 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 (5.08 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 (5.08 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 | 2.0319 mL | 10.1597 mL | 20.3194 mL | |
| 5 mM | 0.4064 mL | 2.0319 mL | 4.0639 mL | |
| 10 mM | 0.2032 mL | 1.0160 mL | 2.0319 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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