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| Targets |
Saperconazole targets the fungal enzyme lanosterol 14α-demethylase (CYP51). This enzyme is a cytochrome P-450 enzyme responsible for the conversion of lanosterol to ergosterol, a critical component of the fungal cell membrane. By inhibiting this enzyme, Saperconazole disrupts the synthesis of ergosterol, leading to a compromised cell membrane and ultimately fungal cell death.
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| ln Vitro |
At a dosage of 1 μg/mL, sarbeconazole exhibited full antifungal efficacy against all Aspergillus niger strains except one. Throughout the course of 14 days of testing, 80% of all strains (85% for Aspergillus fumigatus) showed no growth at all at a dose of 0.1 μg/mL [2].
Saperconazole exhibits potent in vitro antifungal activity. It has an MIC90 of 0.19 mg/L. Its antifungal activity is complete at 1 μg/mL for most strains. Notably, 80% of all strains, including 85% of Aspergillus fumigatus strains, showed no growth at a concentration as low as 0.1 μg/mL over a 14-day test period. This demonstrates its broad-spectrum and potent activity against clinically relevant fungi. |
| ln Vivo |
Every control pigeon that had A infection. fumigatus passed away in two to five days. Their kidneys, liver, spleen, air sacs, and lungs all developed necrotic lesions. These organs have very positive histology and cultures. When given at 2.5 mg/kg, sarconazole proved ineffective; however, at 5 or 10 mg/kg, there was 100% or 92% survival and negative organ cultures, respectively. P igeons showed no signs of drug-related adverse effects [2].
Saperconazole has demonstrated in vivo antifungal activity in animal models. In one study, administration of Saperconazole at 2.5 mg/kg was not active, but when given at 5 or 10 mg/kg, 92% or 100% of the subjects survived, respectively, and organ cultures were negative. This indicates a dose-dependent efficacy in vivo. However, the specific animal model and infection type are not detailed in the provided excerpts. |
| Enzyme Assay |
The in vitro antifungal activity of Saperconazole is typically assessed using standard broth microdilution assays to determine the minimum inhibitory concentration (MIC). The compound is tested against a panel of fungal strains, and the MIC90, the concentration required to inhibit the growth of 90% of the organisms, is determined. In the provided data, the MIC90 against Aspergillus species was found to be 0.19 mg/L. The assay is often conducted over a 14-day period to assess the duration of activity.
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| Cell Assay |
The in vitro activity of Saperconazole is evaluated using cell-based assays with various fungal strains. The antifungal activity is typically assessed by measuring the inhibition of fungal growth in liquid culture. The compound's ability to completely inhibit growth at 1 μg/mL and to prevent growth of 80% of strains at 0.1 μg/mL demonstrates its potent activity in these cell-based systems.
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| Animal Protocol |
In vivo animal experiments have been conducted to evaluate the efficacy of Saperconazole. In these studies, animals were infected with a fungal pathogen and then treated with Saperconazole at various doses (2.5, 5, and 10 mg/kg). The primary endpoints were survival rate and the presence of the fungus in organ cultures. The results showed that doses of 5 and 10 mg/kg provided significant protection, with 92% and 100% survival, respectively, and negative organ cultures.
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| ADME/Pharmacokinetics |
Saperconazole (R66905) has a molecular weight of 672.72 and a molecular formula of C35H38F2N8O4. For research purposes, the powder should be stored at -20°C for up to 3 years, and in solvent at -80°C for up to 1 year. It is shipped with blue ice or at ambient temperature. The compound's relative density is 1.37 g/cm³. It is a research-grade compound with a purity of ≥95%.
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| Toxicity/Toxicokinetics |
Saperconazole is a triazole antifungal agent that was investigated for its potential in treating fungal infections. Although it demonstrated promising potency in preclinical evaluations, it did not advance to widespread clinical use. Today, it primarily serves as a reference compound in antifungal pharmacology and drug-development research. Its safety and toxicity profile, while not detailed here, would have been a factor in its lack of clinical development.
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| References |
[1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83.
[2]. VVan Cutsem J, et al. Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals. Antimicrob Agents Chemother. 1989 Dec;33(12):2063-8 |
| Additional Infomation |
See also: Saperconazole (note moved to).
Saperconazole (CAS#: 110588-57-3) is a broad-spectrum triazole antifungal agent, also known as R66905. It inhibits the fungal enzyme lanosterol 14α-demethylase (CYP51), blocking ergosterol synthesis and disrupting fungal cell membrane integrity. It has potent in vitro activity against Aspergillus species with an MIC90 of 0.19 mg/L and shows dose-dependent efficacy in vivo. Saperconazole is used as a reference compound in antifungal research. |
| Molecular Formula |
C35H38F2N8O4
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|---|---|
| Molecular Weight |
672.73
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| Exact Mass |
672.298
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| CAS # |
110588-57-3
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| PubChem CID |
9809993
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.37g/cm3
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| Boiling Point |
812.5ºC at 760mmHg
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| Melting Point |
189.5°
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| Flash Point |
445.2ºC
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| Vapour Pressure |
1.81E-26mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
4.678
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
49
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C(C)CC)N=CN1C2=CC=C(N3CCN(C4=CC=C(OCC5OC(CN6N=CN=C6)(C7=CC=C(F)C=C7F)OC5)C=C4)CC3)C=C2
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| InChi Key |
HUADITLKOCMHSB-ZPGVKDDISA-N
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| InChi Code |
InChI=1S/C35H38F2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1
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| Chemical Name |
2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one
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| Synonyms |
R66905; SPZ; Saperconazole
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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 : ~25 mg/mL (~37.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.72 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 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 | 1.4865 mL | 7.4324 mL | 14.8648 mL | |
| 5 mM | 0.2973 mL | 1.4865 mL | 2.9730 mL | |
| 10 mM | 0.1486 mL | 0.7432 mL | 1.4865 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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