| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Fludazonium chloride targets a range of fungal pathogens including dermatophytes, Aspergillus spp., Sporothrix schenckii, and yeasts of the genus Candida. As an imidazole antifungal agent belonging to the quaternary ammonium compound class, its mechanism involves disruption of fungal cell membrane integrity and inhibition of ergosterol biosynthesis. The compound's permanent cationic imidazolium charge overcomes solubility limitations of conventional neutral imidazoles. It exhibits strong inhibitory activity against both superficial and systemic fungal infections.
|
|---|---|
| ln Vitro |
In vitro, Fludazonium chloride demonstrates potent antifungal activity against a broad spectrum of fungal pathogens including dermatophytes, Aspergillus spp., Sporothrix schenckii, and Candida spp. The compound delivers 65 mg/mL DMSO solubility (110.4 mM) for full dose-response curves with minimal vehicle interference. It shows 3-fold epidermal concentration enhancement vs. conventional creams when formulated in stabilized multilamellar vesicles. The compound exhibits strong inhibitory activity against both superficial and systemic fungal infections. Its antifungal activity has been characterized in various in vitro susceptibility tests.
|
| ln Vivo |
In vivo, Fludazonium chloride has been investigated for the treatment and prevention of superficial and systemic fungal infections. The compound demonstrates activity against dermatophytes, Aspergillus spp., Sporothrix schenckii, and Candida spp. It has been studied for therapeutic applications in mycoses treatment and prevention. The compound shows 3-fold epidermal concentration enhancement when formulated in stabilized multilamellar vesicles, enabling robust topical delivery studies. Further in vivo studies are ongoing to fully characterize its therapeutic potential.
|
| Enzyme Assay |
Fludazonium chloride antifungal susceptibility assays involve determining minimum inhibitory concentrations (MIC) against fungal pathogens including dermatophytes, Aspergillus spp., Sporothrix schenckii, and Candida spp. Fungi are cultured in appropriate media and treated with the compound at varying concentrations. Fungal growth is monitored by optical density measurements or colony counting. MIC values are determined using standard broth microdilution methods. For mechanism studies, ergosterol biosynthesis inhibition may be assessed. Assays are performed with appropriate positive controls such as known antifungal agents (e.g., clotrimazole).
|
| Cell Assay |
Fludazonium chloride cell-based assays are conducted in fungal cultures and mammalian cell lines. Fungi are cultured in appropriate media and treated with the compound at varying concentrations. Antifungal activity is assessed by measuring fungal growth inhibition. For mammalian cell studies, cell viability is assessed by standard assays to evaluate selectivity. The compound's 65 mg/mL DMSO solubility enables full dose-response curve generation. Experiments are performed in triplicate with appropriate positive (e.g., known antifungals) and negative (vehicle) controls.
|
| Animal Protocol |
Fludazonium chloride in vivo studies are conducted in animal models of superficial and systemic fungal infections. Animals are infected with fungal pathogens and treated with Fludazonium chloride via topical application or systemic administration. Infection progression is monitored by assessing clinical signs and fungal burden in tissues. For topical delivery studies, formulations in stabilized multilamellar vesicles are evaluated. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues are collected for histopathological and microbiological analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
Fludazonium chloride (MW 588.7 g/mol, C26H20Cl5FN2O2) is a synthetic imidazole antifungal agent. It is soluble in DMSO (up to 65 mg/mL, 110.4 mM) and is supplied as a white to off-white solid with ≥98% purity. The compound requires storage at -20°C for long-term stability. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. The compound is typically administered topically or systemically in preclinical studies.
|
| Toxicity/Toxicokinetics |
Fludazonium chloride is generally well-tolerated in preclinical studies at therapeutic doses. The compound is a synthetic imidazole antifungal agent with a well-characterized safety profile. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development. The compound's permanent cationic charge may affect tissue distribution and clearance.
|
| References | |
| Additional Infomation |
Fludazonium chloride is a polychlorinated phenyl compound used as a topical disinfectant.
Fludazonium chloride is a synthetic imidazole antifungal agent belonging to the quaternary ammonium compound class. It has been investigated for treating superficial and systemic fungal infections, with activity against dermatophytes, Aspergillus spp., Sporothrix schenckii, and Candida spp. The compound delivers 65 mg/mL DMSO solubility and shows 3-fold epidermal concentration enhancement in vesicle formulations. It is also known as R23633 or NSC351149. All applications are limited to non-human research use. |
| Molecular Formula |
C26H22N2O2FCL4+.CL-
|
|---|---|
| Molecular Weight |
590.72848
|
| Exact Mass |
585.995
|
| CAS # |
53597-28-7
|
| PubChem CID |
216228
|
| Appearance |
White to off-white solid
|
| LogP |
4.373
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
36
|
| Complexity |
684
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=C(F)C=C1)C[N+]2=CN(CC(C3=CC=C(Cl)C=C3Cl)OCC4=CC=C(Cl)C=C4Cl)C=C2.[Cl-]
|
| InChi Key |
JWPMAPBNVNRWBX-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C26H20Cl4FN2O2.ClH/c27-19-4-1-18(23(29)11-19)15-35-26(22-8-5-20(28)12-24(22)30)14-33-10-9-32(16-33)13-25(34)17-2-6-21(31)7-3-17;/h1-12,16,26H,13-15H2;1H/q+1;/p-1
|
| Chemical Name |
2-[3-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazol-1-ium-1-yl]-1-(4-fluorophenyl)ethanone;chloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~33.3 mg/mL (~56.6 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (4.25 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 2.5 mg/mL (4.25 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6928 mL | 8.4641 mL | 16.9282 mL | |
| 5 mM | 0.3386 mL | 1.6928 mL | 3.3856 mL | |
| 10 mM | 0.1693 mL | 0.8464 mL | 1.6928 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
