| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Fosravuconazole targets fungal CYP51 (lanosterol 14α‑demethylase), a key enzyme in ergosterol synthesis. As a prodrug, it is converted to ravuconazole, which binds to CYP51 and inhibits ergosterol production, compromising fungal cell membrane integrity and leading to cell death.
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|---|---|
| ln Vitro |
Strong in vitro antifungal activity of Ravuconodium has been observed against Candida, Aspergillus, and Trichophyton, among other fungi [1].
In vitro, fosravuconazole (as ravuconazole) exhibits potent antifungal activity against Candida spp., Aspergillus spp., and other fungi, with MIC values in the susceptible range. The prodrug itself has lower activity but is rapidly converted in vivo to the active metabolite. |
| ln Vivo |
In mice infected with the Y strain of Trypanosoma cruzi, treatment with foslaconazole (E-1224; 10-50 mg/kg; oral; daily; for 20 days) lowers parasitemia and averts death [3].
In vivo, fosravuconazole shows comparable efficacy to ravuconazole in a murine Candida albicans infection model upon oral administration; its improved water solubility over ravuconazole enhances bioavailability and allows parenteral formulation, making it useful for invasive fungal infections. |
| Enzyme Assay |
Antifungal activity is assessed by broth microdilution to determine MIC against fungal strains. CYP51 inhibition is measured in cell‑free assays using recombinant fungal CYP51, lanosterol, and NADPH; ergosterol production is quantified by HPLC to confirm the mechanism.
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| Cell Assay |
Cell‑based assays use fungal cultures; growth inhibition is measured after treatment with fosravuconazole or ravuconazole to determine MIC. The prodrug’s activity is compared to the active metabolite to confirm conversion efficacy.
|
| Animal Protocol |
Animal/Disease Models: Swiss female mice (20-24 g) inoculated with trypomastigotes (Y strain) [3].
Doses: 10 mg/kg, 20 mg/kg, 30 mg/kg, 40 mg/kg, 50 mg/kg Route of Administration: Oral; daily; for 20 days Experimental Results: Suppression of parasitemia and prevention of death. In vivo mouse models of candidiasis involve oral or intravenous administration of fosravuconazole; fungal burden in kidneys or other organs is measured. PK studies in rats after i.v. dosing assess prodrug conversion and exposure of ravuconazole. |
| ADME/Pharmacokinetics |
Fosravuconazole (C₂₃H₂₀F₂N₅O₅PS) is a prodrug with enhanced water solubility; it is rapidly converted to ravuconazole in vivo. PK parameters (half‑life, Cmax, AUC) are not fully detailed, but the improved solubility facilitates administration and potentially better bioavailability.
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| Toxicity/Toxicokinetics |
Toxicity data are not fully reported; as an azole antifungal, potential hepatotoxicity, drug interactions (CYP inhibition), and gastrointestinal effects are known class risks. Its prodrug design may improve tolerability, but safety studies are required.
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| References |
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| Additional Infomation |
BMS 379224 is an amine. Fosavoconazole is being studied in the clinical trial NCT03378661 (BENDITA: New Dosage of Bennidazole for Improved Treatment and Relevance).
Fosravuconazole is an investigational antifungal not yet approved; it has been studied for invasive fungal infections, especially in immunocompromised hosts. Its prodrug approach addresses ravuconazole’s poor solubility, and it may offer advantages over other azoles. Further clinical trials are needed. |
| Molecular Formula |
C23H20F2N5O5PS
|
|---|---|
| Molecular Weight |
547.470971107483
|
| Exact Mass |
547.089
|
| CAS # |
351227-64-0
|
| Related CAS # |
Fosravuconazole L-lysine ethanolate;914361-45-8
|
| PubChem CID |
9807507
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
4.334
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
37
|
| Complexity |
859
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C[C@@H](C1=NC(=CS1)C2=CC=C(C=C2)C#N)[C@](CN3C=NC=N3)(C4=C(C=C(C=C4)F)F)OCOP(=O)(O)O
|
| InChi Key |
SYTNEMZCCLUTNX-NPMXOYFQSA-N
|
| InChi Code |
InChI=1S/C23H20F2N5O5PS/c1-15(22-29-21(10-37-22)17-4-2-16(9-26)3-5-17)23(11-30-13-27-12-28-30,34-14-35-36(31,32)33)19-7-6-18(24)8-20(19)25/h2-8,10,12-13,15H,11,14H2,1H3,(H2,31,32,33)/t15-,23+/m0/s1
|
| Chemical Name |
(((2R,3R)-3-(4-(4-cyanophenyl)thiazol-2-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-yl)oxy)methyl dihydrogen phosphate
|
| Synonyms |
Fosravuconazole; BEF-1224; BMS 379224; E-1224; BEF1224; BMS379224; E 1224; BEF 1224; BMS-379224; E1224.
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~182.66 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 | 1.8266 mL | 9.1329 mL | 18.2658 mL | |
| 5 mM | 0.3653 mL | 1.8266 mL | 3.6532 mL | |
| 10 mM | 0.1827 mL | 0.9133 mL | 1.8266 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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