| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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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].
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|---|---|
| ln Vivo |
Neticonazole (1–100 ng/kg; administered daily for 15 days via lateral gavage; for cosmetic C57BL/6 hair) dramatically enhances xenografts of colorectal cancer (CRC) that are contaminated with bacterial toxin (IDB).
|
| 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. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8 weeks old) 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 the survival of IDB mice with CRC xenograft tumors. |
| References |
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| Additional Infomation |
Neticonazole is an enamine that is ethene which is substituted at positions 1, 1, and 2 by o-pentoxyphenyl, 1H-imidazol-1-yl, and methylthio groups, respectively (the E isomer). An inhibitor of P450-dependent C-14alpha-demethylation of lanosterol (preventing conversion to ergosterol and inhibiting cell wall synthesis in fungi), it is used in Japan (generally as the corresponding hydrochloride salt) as an antifungal drug for the treatment of superficial skin infections. It has a role as an antifungal drug and an EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor. It is an aromatic ether, a methyl sulfide, a member of imidazoles, an enamine, a member of benzenes, a conazole antifungal drug and an imidazole antifungal drug. It is a conjugate base of a neticonazole(1+).
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| Molecular Formula |
C17H22N2OS
|
|---|---|
| Molecular Weight |
302.43438
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| Exact Mass |
302.145
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| CAS # |
130726-68-0
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| Related CAS # |
Neticonazole hydrochloride;130773-02-3
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| PubChem CID |
5282433
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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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| Index of Refraction |
1.558
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| LogP |
4.661
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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 |
8
|
| Heavy Atom Count |
21
|
| Complexity |
322
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCCCOC1=CC=CC=C1/C(=C\SC)/N2C=CN=C2
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| InChi Key |
VWOIKFDZQQLJBJ-DTQAZKPQSA-N
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| InChi Code |
InChI=1S/C17H22N2OS/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/b16-13+
|
| Chemical Name |
1-[(E)-2-methylsulfanyl-1-(2-pentoxyphenyl)ethenyl]imidazole
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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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~826.64 mM)
1M HCl : 100 mg/mL (~330.66 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (20.67 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. Solubility in Formulation 2: ≥ 6.25 mg/mL (20.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3066 mL | 16.5328 mL | 33.0655 mL | |
| 5 mM | 0.6613 mL | 3.3066 mL | 6.6131 mL | |
| 10 mM | 0.3307 mL | 1.6533 mL | 3.3066 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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