Flusilazole
Based on 1 Customer Validation
Flusilazole (DPX-H6573) is a broad-spectrum fungicide and cytochrome P-450 inhibitor that can be used in studies related to fungal infections.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.82%
- CAS No.: 85509-19-9
- 화학식: C16H15F2N3Si
- 분자량:315.39
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Flusilazole (DPX-H6573) binds to cytochrome P-450 in Saccharomyces cerevisiae microsomes (Kd = 21 nM), partially purified Saccharomyces cerevisiae lanosterol 14α-demethylase (Kd = 22 nM), rat liver microsomes (Kd = 496 nM), and purified rat liver P-45014DM (Kd = 45 nM), with comparable binding affinity between purified yeast and rat liver target demethylase enzymes[2].
Flusilazole (5 μM) inhibits cholesterol 7α-hydroxylase activity in rat liver microsomes with an IC50 of 5 μM[2].
Flusilazole (0.01-100 μM) induces accumulation of lanosterol demethylase oxysterol intermediates in microsomal preparations, with peak accumulation of 0.2 nanomoles at a concentration of 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 85509-19-9
-
Appearance Solid
-
분자량 315.39
-
화학식 C16H15F2N3Si
-
Color White to off-white
-
SMILES
C[Si](CN1N=CN=C1)(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3
-
Synonyms
DPX-H6573
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (317.07 mM; Need ultrasonic; 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
순도&문서
-
Data Sheet (276 KB)
-
SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
-
Handling Instructions (2659 KB)
References
[1]. Mercado DF, et al. Reaction kinetics and mechanisms of organosilicon fungicide flusilazole with sulfate and hydroxyl radicals. Chemosphere. 2018;190:327-336. [Content Brief]
[2]. Trzaskos JM, Henry MJ. Comparative effects of the azole-based fungicide flusilazole on yeast and mammalian lanosterol 14 alpha-methyl demethylase. Antimicrob Agents Chemother. 1989 Aug;33(8):1228-31. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1707 mL | 15.8534 mL | 31.7068 mL | 79.2669 mL |
| 5 mM | 0.6341 mL | 3.1707 mL | 6.3414 mL | 15.8534 mL | |
| 10 mM | 0.3171 mL | 1.5853 mL | 3.1707 mL | 7.9267 mL | |
| 15 mM | 0.2114 mL | 1.0569 mL | 2.1138 mL | 5.2845 mL | |
| 20 mM | 0.1585 mL | 0.7927 mL | 1.5853 mL | 3.9633 mL | |
| 25 mM | 0.1268 mL | 0.6341 mL | 1.2683 mL | 3.1707 mL | |
| 30 mM | 0.1057 mL | 0.5284 mL | 1.0569 mL | 2.6422 mL | |
| 40 mM | 0.0793 mL | 0.3963 mL | 0.7927 mL | 1.9817 mL | |
| 50 mM | 0.0634 mL | 0.3171 mL | 0.6341 mL | 1.5853 mL | |
| 60 mM | 0.0528 mL | 0.2642 mL | 0.5284 mL | 1.3211 mL | |
| 80 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL | |
| 100 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL | 0.7927 mL |
- Flusilazole
- 85509-19-9
- DPX-H6573
- Environmental Pollutants
- Fungal
- cholesterol biosynthesis
- lanosterol 14α-demethylase
- yeast lanosterol 14α-methyl demethylase
- fungal infections
- rodent models
- cytochrome P-450
- Saccharomyces cerevisiae
- rat liver lanosterol 14α-methyl demethylase
- higher plant models
- rat liver cholesterol 7α-hydroxylase
- Inhibitor
- inhibitor
- inhibit