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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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Fosravuconazole L-lysine ethanolate is the L-lysine ethanolate salt form of Fosravuconazole. Fosravuconazole (E1224; BEF1224; BMS379224) is an azole antifungal agent used for the treatment of fungal infections. It is a prodrug of ravuconazole with improved water solubility.
| ln Vitro |
Aspergillus, Candida, and Trichophyton species are only a few of the many fungus species that Fosravuconodium effectively inhibits in vitro [1].
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|---|---|
| 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].
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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. |
| 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. |
| 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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