Fosravuconazole
Based on 1 Customer Validation
Fosravuconazole (BMS-379224), a proagent of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole can be used for candidiasis, onychomycosis and parasitemia research.
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- Pureza: 99.86%
- No. CAS: 351227-64-0
- Fòrmula: C23H20F2N5O5PS
- Peso molecular:547.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
Fungal[1]
Ravuconazole has potent in vitro antifungal activity against a wide range of fungal species, including Candida, Aspergillus, and Trichophyton species[1].
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.
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Animal Model:Swiss female mice (20-24 g) inoculated with trypomastigotes (Y strain)[3].
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Dosage:10 mg/kg, 20 mg/kg, 30 mg/kg, 40 mg/kg, 50 mg/kg
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Administration:Oral administration; daily; for 20 days
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Result:Suppressed the parasitemia and prevented death.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 351227-64-0
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Appearance Solid
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Peso molecular 547.47
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Fòrmula C23H20F2N5O5PS
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Color White to light yellow
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SMILES
N#CC1=CC=C(C2=CSC([C@H](C)[C@@](OCOP(O)(O)=O)(C3=CC=C(F)C=C3F)CN4N=CN=C4)=N2)C=C1
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Synonyms
BMS-379224; E-1224
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (182.66 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 (4.57 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 (4.57 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:
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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.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shinichi Watanabe, et al. Efficacy and safety of fosravuconazole L-lysine ethanolate, a novel oral triazole antifungal agent, for the treatment of onychomycosis: A multicenter, double-blind, randomized phase III study. J Dermatol. 2018 Oct;45(10):1151-1159. [Content Brief]
[2]. Katsura Hata, et al. Development of E1224 by leveraging a strategic partnership for the medicines creation against neglected tropical diseases. Parasitol Int. 2020 Dec 25;81:102278. [Content Brief]
[3]. Lívia de Figueiredo Diniz, et al. Outcome of E1224-Benznidazole Combination Treatment for Infection with a Multidrug-Resistant Trypanosoma cruzi Strain in Mice. Antimicrob Agents Chemother. 2018 May 25;62(6):e00401-18. [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 | 1.8266 mL | 9.1329 mL | 18.2658 mL | 45.6646 mL |
| 5 mM | 0.3653 mL | 1.8266 mL | 3.6532 mL | 9.1329 mL | |
| 10 mM | 0.1827 mL | 0.9133 mL | 1.8266 mL | 4.5665 mL | |
| 15 mM | 0.1218 mL | 0.6089 mL | 1.2177 mL | 3.0443 mL | |
| 20 mM | 0.0913 mL | 0.4566 mL | 0.9133 mL | 2.2832 mL | |
| 25 mM | 0.0731 mL | 0.3653 mL | 0.7306 mL | 1.8266 mL | |
| 30 mM | 0.0609 mL | 0.3044 mL | 0.6089 mL | 1.5222 mL | |
| 40 mM | 0.0457 mL | 0.2283 mL | 0.4566 mL | 1.1416 mL | |
| 50 mM | 0.0365 mL | 0.1827 mL | 0.3653 mL | 0.9133 mL | |
| 60 mM | 0.0304 mL | 0.1522 mL | 0.3044 mL | 0.7611 mL | |
| 80 mM | 0.0228 mL | 0.1142 mL | 0.2283 mL | 0.5708 mL | |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1827 mL | 0.4566 mL |