| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Sulconazole targets fungal cytochrome P-450 sterol C-14 alpha-demethylase, a key enzyme in the ergosterol biosynthesis pathway. By inhibiting this enzyme, sulconazole blocks the conversion of lanosterol to ergosterol, leading to the accumulation of toxic 14α-methyl sterols and depletion of ergosterol. This disrupts the integrity of the fungal cell membrane, resulting in cell death.
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| ln Vitro |
At doses less than 5 mg/L in vitro, succinazole mononitrate exhibits broad-spectrum antifungal action and can impede the growth of yeasts, dermatophytes, and a variety of filamentous and dimorphic fungi [1]. With a minimum inhibitory concentration (MIC) of less than 12.5 mg/L, succinazole mononitrate has antibacterial activity in vitro against several strains of Staphylococcus aureus, Streptococcus faecalis, and some Gram-positive anaerobic bacteria [1].
In vitro, sulconazole nitrate possesses a broad spectrum of activity against dermatophytes, yeasts, and some Gram-positive bacteria. It has activity against Malassezia furfur and Candida albicans. Its antifungal activity is well-characterized. |
| ln Vivo |
In vivo, sulconazole nitrate is used for the topical treatment of dermatophyte infections such as tinea corporis and tinea cruris. It is applied topically as a cream or solution. It is effective against a variety of fungal pathogens.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for sulconazole nitrate typically involve evaluating its inhibitory activity against fungal cytochrome P-450 sterol C-14 alpha-demethylase. The enzyme is incubated with varying concentrations of sulconazole and its substrate. The reaction is monitored by measuring the accumulation of 14α-methyl sterols or the depletion of ergosterol, and the IC₅₀ is determined.
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| Cell Assay |
For in vitro cell-based assays, sulconazole nitrate is dissolved in DMSO and applied to cultured fungal cells at concentrations ranging from 0.1-100 µg/mL. The Minimum Inhibitory Concentration (MIC) is determined using standard broth dilution methods. The effects on fungal cell growth and membrane integrity are assessed.
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| Animal Protocol |
In vivo animal studies for sulconazole nitrate are typically conducted in guinea pig or mouse models of dermatophyte infection. Sulconazole nitrate is applied topically at concentrations ranging from 0.1-1%. Efficacy is evaluated by measuring the reduction in fungal load and the resolution of skin lesions.
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| ADME/Pharmacokinetics |
Sulconazole nitrate has a molecular formula of C₁₈H₁₅Cl₃N₂S·HNO₃ and a molecular weight of 460.77 g/mol. It is a white to off-white powder with a melting point of 130.5-132°C. It is soluble in DMSO and is typically stored at room temperature.
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| Toxicity/Toxicokinetics |
Sulconazole nitrate is considered to have a manageable toxicity profile for topical use. As a topical antifungal, systemic absorption is limited. Common side effects may include local irritation and hypersensitivity reactions.
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| References | |
| Additional Infomation |
Sulconazole nitrate is an organic nitrate belonging to the conazole and imidazole classes of antifungal drugs. Sulconazole nitrate is the nitrate form of Sulconazole, a synthetic imidazole derivative with antifungal activity. Sulconazole nitrate inhibits the C-14α-demethylation of fungal cytochrome P-450 sterols, leading to the accumulation of 14α-methylsterol in fungi, and inhibits the synthesis of ergosterol (an important component of the fungal cell membrane). Inhibition of ergosterol synthesis leads to disruption of cell membrane permeability, ultimately inhibiting cell wall synthesis. Furthermore, Sulconazole nitrate appears to interfere with the autolytic degradation of fungal DNA and RNA. See also: Sulconazole (containing the active moiety).
Sulconazole nitrate is an imidazole antifungal agent used for the topical treatment of dermatophyte infections. It is also known as RS 44872. Sulconazole nitrate is approved for clinical use in some countries. It is supplied by various pharmaceutical and research chemical suppliers for human and research use. |
| Molecular Formula |
C18H16CL3N3O3S
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|---|---|
| Molecular Weight |
460.7619
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| Exact Mass |
458.998
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| CAS # |
61318-91-0
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| Related CAS # |
Sulconazole;61318-90-9
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| PubChem CID |
65495
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| Appearance |
White to off-white solid powder
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| Boiling Point |
558.2ºC at 760 mmHg
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| Melting Point |
130.5-132℃
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| Flash Point |
291.4ºC
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| LogP |
6.693
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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 |
28
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| Complexity |
404
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1CSC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl.[N+](=O)(O)[O-]
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| InChi Key |
CRKGMGQUHDNAPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15Cl3N2S.HNO3/c19-14-3-1-13(2-4-14)11-24-18(10-23-8-7-22-12-23)16-6-5-15(20)9-17(16)212-1(3)4/h1-9,12,18H,10-11H2(H,2,3,4)
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| Chemical Name |
1-(2-((4-chlorobenzyl)thio)-2-(2,4-dichlorophenyl)ethyl)-1H-imidazole nitrate
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| Synonyms |
Sulconazole RS-44872 RS 44872 RS44872 Exelderm
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~271.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.51 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 20.8 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: ≥ 2.08 mg/mL (4.51 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 20.8 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: ≥ 2.08 mg/mL (4.51 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 | 2.1703 mL | 10.8516 mL | 21.7033 mL | |
| 5 mM | 0.4341 mL | 2.1703 mL | 4.3407 mL | |
| 10 mM | 0.2170 mL | 1.0852 mL | 2.1703 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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