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| 10mg |
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| Targets |
Fosravuconazole L-lysine ethanolate targets fungal lanosterol 14α-demethylase, an enzyme in the ergosterol biosynthesis pathway. As a prodrug, it is converted to ravuconazole, the active triazole antifungal agent. Ravuconazole inhibits lanosterol 14α-demethylase, blocking ergosterol synthesis and disrupting fungal cell membrane integrity.
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| ln Vitro |
Aspergillus, Candida, and Trichophyton species are only a few of the many fungus species that Fosravuconodium effectively inhibits in vitro [1].
In vitro, fosravuconazole is a prodrug that is converted to ravuconazole. Ravuconazole has potent in vitro antifungal activity against a wide range of fungal species, including Candida, Aspergillus, and Trichophyton species. Its activity is assessed by determining the minimum inhibitory concentration (MIC) against various fungal strains. |
| 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 L-lysine ethanolate is orally active. It increases survival in a mouse model of systemic C. albicans infection. It is used for research on candidiasis, onychomycosis, and parasitemia. The prodrug formulation enhances the oral bioavailability of ravuconazole. |
| Enzyme Assay |
In vitro enzyme assays for fosravuconazole are not typically performed. Its activity is assessed through its conversion to ravuconazole and the subsequent inhibition of fungal lanosterol 14α-demethylase. Ravuconazole's antifungal activity is characterized by MIC determinations.
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| Cell Assay |
In vitro cell-based assays for fosravuconazole involve testing its antifungal activity against a panel of fungal strains. The compound is added to fungal cultures, and growth inhibition is measured. Its activity is compared to that of ravuconazole and other antifungal agents.
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| 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 animal experiments for fosravuconazole L-lysine ethanolate have been conducted in a mouse model of systemic C. albicans infection. Mice are infected with C. albicans and treated with the compound orally. Efficacy is measured by survival rates and reduction in fungal burden in organs. |
| ADME/Pharmacokinetics |
Fosravuconazole L-lysine ethanolate is a prodrug of ravuconazole. It is an orally active broad-spectrum antifungal agent. It is also known as BMS-379224 L-lysine ethanolate. It is used for research on fungal infections. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Fosravuconazole L-lysine ethanolate is for research use only and is not intended for human use. Its safety profile is being evaluated in preclinical studies. Standard safety precautions should be taken when handling.
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| References |
[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.
[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. [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. |
| Additional Infomation |
Fosravuconazole L-lysine ethanolate is an orally active broad-spectrum antifungal prodrug of ravuconazole. It is used for research on candidiasis, onychomycosis, and parasitemia. It increases survival in a mouse model of systemic C. albicans infection. It is also known as BMS-379224 L-lysine ethanolate.
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| Molecular Formula |
C31H40F2N7O8PS
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|---|---|
| Molecular Weight |
739.72697353363
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| Exact Mass |
739.236
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| Elemental Analysis |
C, 50.33; H, 5.45; F, 5.14; N, 13.25; O, 17.30; P, 4.19; S, 4.33
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| CAS # |
914361-45-8
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| Related CAS # |
Fosravuconazole;351227-64-0
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| PubChem CID |
112499965
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
50
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| Complexity |
967
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCO.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.C(CCN)C[C@@H](C(=O)O)N
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| InChi Key |
VOWYGLHOVNSCSA-NRVKWRQJSA-N
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| InChi Code |
InChI=1S/C23H20F2N5O5PS.C6H14N2O2.C2H6O/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;7-4-2-1-3-5(8)6(9)10;1-2-3/h2-8,10,12-13,15H,11,14H2,1H3,(H2,31,32,33);5H,1-4,7-8H2,(H,9,10);3H,2H2,1H3/t15-,23+;5-;/m00./s1
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| Chemical Name |
[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1,2,4-triazol-1-yl)butan-2-yl]oxymethyl dihydrogen phosphate;(2S)-2,6-diaminohexanoic acid;ethanol
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| Synonyms |
BFE 1224 BFE1224 E-1224 BEF-1224 BMS-379224 BEF 1224 BMS 379224Fosravuconazole L-lysine ethanolate
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| HS Tariff Code |
2934.99.03.00
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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, avoid exposure to moisture. |
| 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) |
H2O : ~200 mg/mL (~270.37 mM)
DMSO : ~50 mg/mL (~67.59 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.38 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 (3.38 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: 50 mg/mL (67.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3518 mL | 6.7592 mL | 13.5184 mL | |
| 5 mM | 0.2704 mL | 1.3518 mL | 2.7037 mL | |
| 10 mM | 0.1352 mL | 0.6759 mL | 1.3518 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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