| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Neticonazole HCl targets fungal cytochrome P450-dependent 14α-demethylase (lanosterol C-14α-demethylase), a key enzyme in the ergosterol biosynthesis pathway. By inhibiting this enzyme, it prevents the conversion of lanosterol to ergosterol, an essential component of fungal cell membranes. In addition to its antifungal target, neticonazole has been shown to modulate exosome secretion pathways, affecting proteins such as Alix, Rab27a, and nSMase2 in cancer cells. This dual targeting of fungal sterol synthesis and mammalian exosome pathways underlies its broad biological activities.
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| ln Vitro |
Treatment with neticonazole (10 μM; 48 h) decreased the levels of Alix and Rab27a and markedly decreased the levels of nSMase2. Significant p-ERK level inhibition is possible with neticonazole [2]. Exosome release from C4-2B cells is potently and dose-dependently inhibited by neticonazole (0–10 μM) [2]. Additionally, neticonazole has an aqueous solution-dependent, biogenic wound-active exosome [3].
In vitro, treatment with neticonazole (10 μM; 48 hours) decreased the levels of Alix and Rab27a and markedly decreased the levels of nSMase2 in C4-2B cells. Significant p-ERK level inhibition is also possible with neticonazole. Exosome release from C4-2B cells is potently and dose-dependently inhibited by neticonazole (0–10 μM). The compound has demonstrated anti-infectious effects and aqueous solution-dependent, biogenic wound-active exosome activity. As an imidazole derivative, it serves as a valuable tool for investigating antifungal mechanisms and resistance pathways. |
| ln Vivo |
Neticonazole hydrochloride treatment (1–100 ng/kg; lateral wall tube feeding; once daily; C57BL/6 mice; formulated) increased the contaminating bacterial flora (IDB) cleanup in rats with rectal cancer (CRC) considerably. Tumor xenograft
In vivo, neticonazole hydrochloride treatment (1–100 ng/kg; oral gavage; once daily for 15 days) in C57BL/6 mice significantly improved survival of mice with colorectal cancer xenograft tumors. The treatment also increased the clearance of contaminating bacterial flora in the gut. In a mouse model where animals were given antibiotics and injected with SW480 cells, neticonazole dramatically improved survival of mice with CRC xenograft tumors. These findings suggest that neticonazole's inhibition of exosome release may contribute to its anti-tumor efficacy in vivo. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays typically involve assessing the compound's inhibition of cytochrome P450-dependent 14α-demethylase activity. Fungal microsomal preparations are incubated with radiolabeled lanosterol or other sterol substrates in the presence of neticonazole, and the conversion to ergosterol is measured by chromatographic methods. IC50 values for enzyme inhibition can be determined by quantifying the accumulation of 14α-methylated sterols. The compound's binding affinity to the enzyme's active site can be evaluated using spectrophotometric assays that measure the interaction with the heme iron of the cytochrome P450 enzyme.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: C4 -2B Cell Tested Concentrations: 10 µM Incubation Duration: 48 hrs (hours) Experimental Results: diminished Alix and Rab27a levels, and Dramatically diminished nSMase2 levels. Neticonazole is evaluated in cell-based assays using fungal and mammalian cell lines. For antifungal activity, broth microdilution assays are performed according to CLSI guidelines to determine minimum inhibitory concentrations (MICs) against various fungal strains including dermatophytes and Candida species. For anti-cancer activity, C4-2B prostate cancer cells or other cancer cell lines are treated with neticonazole (0–10 μM) for 48 hours, followed by Western blot analysis to assess protein levels of Alix, Rab27a, and nSMase2. Exosome release is quantified by nanoparticle tracking analysis or by measuring exosomal markers in conditioned media. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8 weeks old) were given ampicillin, neomycin, metronidazole and vancomycin, and injected with SW480 cells [3].
Doses: 1 ng/kg, 10 ng/kg, and 100 ng/kg Route of Administration: po (oral gavage); daily; for 15 days Experimental Results: Dramatically improved survival of IDB mice with CRC xenograft tumors. In vivo animal studies typically use mouse models. In a colorectal cancer xenograft model, male C57BL/6 mice (8 weeks old) are first administered antibiotics (ampicillin, neomycin, metronidazole, vancomycin) to deplete the gut microbiota, then injected with SW480 cancer cells. Neticonazole hydrochloride is administered orally at doses of 1, 10, or 100 ng/kg once daily for 15 days. Endpoints include survival analysis, tumor growth measurement, and assessment of gut bacterial flora clearance. Alternative models include topical application for superficial fungal infection studies. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of neticonazole hydrochloride are not extensively documented in publicly available literature. As a topical and oral antifungal agent, it is characterized by long-acting properties. The compound has a molecular weight of 338.90 g/mol and a logP of 5.463, indicating high lipophilicity. It is a hydrochloride salt formed by reacting equimolar amounts of neticonazole with hydrogen chloride. For research use, the compound is typically stored at -20°C and formulated in appropriate vehicles for in vivo administration.
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| Toxicity/Toxicokinetics |
Neticonazole hydrochloride is generally well-tolerated at research doses. In mouse studies, oral administration at doses up to 100 ng/kg for 15 days did not report significant adverse effects. As an imidazole antifungal, it may share class-related toxicities including potential hepatotoxicity and drug-drug interactions mediated by cytochrome P450 inhibition. However, specific toxicological data for neticonazole hydrochloride in preclinical models are limited in publicly available sources. For research use only, not for therapeutic or human use.
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| References |
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| Additional Infomation |
Neteconazole hydrochloride is a hydrochloride salt formed by reacting an equimolar amount of neteconazole with hydrogen chloride. It is a P450-dependent lanosterol C-14α-demethylation inhibitor (preventing the conversion of lanosterol to ergosterol and inhibiting fungal cell wall synthesis), and is used in Japan as an antifungal drug for treating superficial skin infections. It is both an antifungal drug and an EC 1.14.13.70 (sterol 14α-demethylase) inhibitor. It is a hydrochloride salt belonging to the imidazole and conazole antifungal classes. It contains neteconazole (1+).
Neticonazole hydrochloride (CAS# 130773-02-3) is an imidazole analogue with dual antifungal and anti-cancer activities. It is a P450-dependent lanosterol C-14α-demethylation inhibitor and is used in Japan as an antifungal drug for treating superficial skin infections. It is both an antifungal drug and an EC 1.14.13.70 (sterol 14α-demethylase) inhibitor. It is a hydrochloride salt belonging to the imidazole and conazole antifungal classes. The compound has been cited in research for its effects on exosome release and cancer cell signaling pathways. The related CAS number for the free base is 130726-68-0. |
| Molecular Formula |
C17H22N2OS.HCL
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| Molecular Weight |
338.8953
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| Exact Mass |
338.122
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| CAS # |
130773-02-3
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| Related CAS # |
Neticonazole;130726-68-0
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| PubChem CID |
5282432
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| Appearance |
White to off-white solid powder
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| Density |
1.06g/cm3
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| Boiling Point |
464ºC at 760mmHg
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| Flash Point |
234.4ºC
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| Vapour Pressure |
8.66E-09mmHg at 25°C
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| LogP |
5.463
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
322
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCOC1=CC=CC=C1/C(=C\SC)/N2C=CN=C2.Cl
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| InChi Key |
HAHMABKERDVYCH-ZUQRMPMESA-N
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| InChi Code |
InChI=1S/C17H22N2OS.ClH/c1-3-4-7-12-20-17-9-6-5-8-15(17)16(13-21-2)19-11-10-18-14-19;/h5-6,8-11,13-14H,3-4,7,12H2,1-2H3;1H/b16-13+;
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| Chemical Name |
1-[(E)-2-methylsulfanyl-1-(2-pentoxyphenyl)ethenyl]imidazole;hydrochloride
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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 : ~250 mg/mL (~737.68 mM)
H2O : ≥ 100 mg/mL (~295.07 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (18.44 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 62.5 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: ≥ 6.25 mg/mL (18.44 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 62.5 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: ≥ 6.25 mg/mL (18.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (295.07 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9507 mL | 14.7536 mL | 29.5072 mL | |
| 5 mM | 0.5901 mL | 2.9507 mL | 5.9014 mL | |
| 10 mM | 0.2951 mL | 1.4754 mL | 2.9507 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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