Saperconazole
Based on 1 Customer Validation
Saperconazole (R66905) is a broad-spectrum antifungal triazole and has potent activity against Aspergillus with an MIC90 of 0.19 mg/L.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 110588-57-3
- Formula: C35H38F2N8O4
- Molecular Weight:672.72
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
MIC90: 0.19 mg/L[1]
The antifungal activity of Saperconazole is complete at 1 μg/mL for all but one strain of A. niger. Eighty percent of all strains show complete absence of growth at 0.1 μg/mL (85% for A. fumigatus), and this result persists during 14 days of the test[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 110588-57-3
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Appearance Solid
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Molecular Weight 672.72
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Formula C35H38F2N8O4
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Color Off-white to light yellow
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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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Synonyms
R66905
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 25 mg/mL (37.16 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
A total of 279 Aspergillus isolates are tested in vitro; 221 of these are A. fumigatus. The inoculum consists of a standardized 4 mm2 culture block containing hyphae and spores for tubes with 5 mL of medium supplemented with drug solution or with solvent[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male immunocompetent (normal) or immunocompromised pigs weighing 500 g (±50 g) are infected intravenously (i.v.) with 25,000 CFU of A.fumigatus B19119 per g of body weight. The animals are treated orally with Saperconazole, ketoconazole, or fluconazole dissolved in polyethylene glycol 200 (PEG 200). The treatment is given once daily for 14 consecutive days, starting on the day of infection or on day 1, 2, 3, or 4 after infection. Saperconazole, dissolved in dimethyl-β-cyclodextrin and in hydroxypropyl-β-cyclodextrin is also administered i.p. and i.v. Pigeons with a mean weight of 400 g (±30 g) are infected i.v. in a wing vein with 7,800 CFU of A.fumigatus B19119 per g of body weight. Saperconazole dissolved in PEG 200 is administered by gavage at 0, 2.5, 5, or 10 mg/kg starting on the day of infection and continued once daily for 14 consecutive days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.4865 mL | 7.4325 mL | 14.8650 mL | 37.1626 mL |
| 5 mM | 0.2973 mL | 1.4865 mL | 2.9730 mL | 7.4325 mL | |
| 10 mM | 0.1487 mL | 0.7433 mL | 1.4865 mL | 3.7163 mL | |
| 15 mM | 0.0991 mL | 0.4955 mL | 0.9910 mL | 2.4775 mL | |
| 20 mM | 0.0743 mL | 0.3716 mL | 0.7433 mL | 1.8581 mL | |
| 25 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4865 mL | |
| 30 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2388 mL |
Saperconazole Related Classifications
HY-U00249 Related Classifications
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