WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H564300
CAS#: 914361-45-8 (L-lysine ethanolate)
Description: Fosravuconazole, also known as E1224, BFE1224 and BMS379224, is a broad-spectrum antifungal agent. In Japan, it is approved for the treatment of onychomycosis, a fungal infection of the nail. It is a prodrug that is converted into ravuconazole.
Hodoodo Cat#: H564300
Name: Fosravuconazole L-lysine ethanolate
CAS#: 914361-45-8 (L-lysine ethanolate)
Chemical Formula: C31H40F2N7O8PS
Exact Mass: 0.00
Molecular Weight: 739.733
Elemental Analysis: C, 50.33; H, 5.45; F, 5.14; N, 13.25; O, 17.30; P, 4.19; S, 4.33
Related CAS #: 351227-64-0 (free base) 914361-44-7 (monolysine) 914361-45-8 (L-lysine ethanolate)
Synonym: Fosravuconazole L-lysine ethanolate; E 1224; E-1224; E1224; BFE1224; BFE 1224; BFE-1224; BMS379224; BMS 379224; BMS-379224; Nailin;
IUPAC/Chemical Name: L-lysine compound with [(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 (1:1:1)
InChi Key: VOWYGLHOVNSCSA-GBTIKMTQSA-N
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-;;/m0../s1
SMILES Code: N[C@@H](CCCCN)C(O)=O.O=P(O)(OCO[C@@](C1=CC=C(C=C1F)F)(CN2N=CN=C2)[C@@H](C)C3=NC(C4=CC=C(C=C4)C#N)=CS3)O.CCO
Appearance: Solid powder
Purity: >95% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 739.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Hata K. Development of E1224 by leveraging a strategic partnership for the medicines creation against neglected tropical diseases. Parasitol Int. 2020 Dec 25;81:102278. doi: 10.1016/j.parint.2020.102278. Epub ahead of print. PMID: 33370607.
2: García M, Kokkinou E, Carrasco García A, Parrot T, Palma Medina LM, Maleki KT, Christ W, Varnaitė R, Filipovic I, Ljunggren HG, Björkström NK, Folkesson E, Rooyackers O, Eriksson LI, Sönnerborg A, Aleman S, Strålin K, Gredmark-Russ S, Klingström J, Mjösberg J; Karolinska KI/K COVID‐19 Study Group. Innate lymphoid cell composition associates with COVID-19 disease severity. Clin Transl Immunology. 2020 Dec 14;9(12):e1224. doi: 10.1002/cti2.1224. PMID: 33343897; PMCID: PMC7734472.
3: Kent A. Toy Models of Top Down Causation. Entropy (Basel). 2020 Oct 27;22(11):E1224. doi: 10.3390/e22111224. PMID: 33286992.
4: Prattapong P, Ngernsombat C, Aimjongjun S, Janvilisri T. CRISPR/Cas9-mediated double knockout of SRPK1 and SRPK2 in a nasopharyngeal carcinoma cell line. Cancer Rep (Hoboken). 2020 Apr;3(2):e1224. doi: 10.1002/cnr2.1224. Epub 2019 Nov 27. PMID: 32671994.
5: Song F, Lang M, Li L, Luo H, Hou Y. Forensic features and genetic background exploration of a new 47-autosomal InDel panel in five representative Han populations residing in Northern China. Mol Genet Genomic Med. 2020 May;8(5):e1224. doi: 10.1002/mgg3.1224. Epub 2020 Mar 10. PMID: 32396282; PMCID: PMC7216812.
6: Hassan S, Channar PA, Larik FA, Saeed A, Shah HS, Lecka J, Sévigny J, Iqbal J. Synthesis of novel (E)-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5'-nucleotidase inhibitors. R Soc Open Sci. 2018 Sep 12;5(9):180837. doi: 10.1098/rsos.180837. PMID: 30839737; PMCID: PMC6170555.
7: Parrado R, Ramirez JC, de la Barra A, Alonso-Vega C, Juiz N, Ortiz L, Illanes D, Torrico F, Gascon J, Alves F, Flevaud L, Garcia L, Schijman AG, Ribeiro I. Usefulness of Serial Blood Sampling and PCR Replicates for Treatment Monitoring of Patients with Chronic Chagas Disease. Antimicrob Agents Chemother. 2019 Jan 29;63(2):e01191-18. doi: 10.1128/AAC.01191-18. PMID: 30509941; PMCID: PMC6355557.
8: Diniz LF, Mazzeti AL, Caldas IS, Ribeiro I, Bahia MT. 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. doi: 10.1128/AAC.00401-18. PMID: 29555633; PMCID: PMC5971593.
9: Torrico F, Gascon J, Ortiz L, Alonso-Vega C, Pinazo MJ, Schijman A, Almeida IC, Alves F, Strub-Wourgaft N, Ribeiro I; E1224 Study Group. Treatment of adult chronic indeterminate Chagas disease with benznidazole and three E1224 dosing regimens: a proof-of-concept, randomised, placebo-controlled trial. Lancet Infect Dis. 2018 Apr;18(4):419-430. doi: 10.1016/S1473-3099(17)30538-8. Epub 2018 Jan 16. PMID: 29352704.
10: Ramírez JC, Parrado R, Sulleiro E, de la Barra A, Rodríguez M, Villarroel S, Irazu L, Alonso-Vega C, Alves F, Curto MA, García L, Ortiz L, Torrico F, Gascón J, Flevaud L, Molina I, Ribeiro I, Schijman AG. First external quality assurance program for bloodstream Real-Time PCR monitoring of treatment response in clinical trials of Chagas disease. PLoS One. 2017 Nov 27;12(11):e0188550. doi: 10.1371/journal.pone.0188550. PMID: 29176887; PMCID: PMC5703561.
11: Moreira PS, Marques P, Soriano-Mas C, Magalhães R, Sousa N, Soares JM, Morgado P. The neural correlates of obsessive-compulsive disorder: a multimodal perspective. Transl Psychiatry. 2017 Aug 29;7(8):e1224. doi: 10.1038/tp.2017.189. PMID: 28850108; PMCID: PMC5611752.
12: Thoma B, Gottlieb M, Boysen-Osborn M, King A, Quinn A, Krzyzaniak S, Pineda N, Yarris LM, Chan T. Curated Collections for Educators: Five Key Papers about Program Evaluation. Cureus. 2017 May 4;9(5):e1224. doi: 10.7759/cureus.1224. PMID: 28589073; PMCID: PMC5453746.
13: Rauso R. Comments on: "Intralipotherapy, the State of the Art". Plast Reconstr Surg Glob Open. 2017 Feb 24;5(2):e1224. doi: 10.1097/GOX.0000000000001224. PMID: 28280666; PMCID: PMC5340481.
14: Yamaguchi H. Potential of Ravuconazole and its Prodrugs as the New OralTherapeutics for Onychomycosis. Med Mycol J. 2016;57(4):E93-E110. doi: 10.3314/mmj.16-00006. PMID: 27904057.
15: Menna-Barreto RF, de Castro SL. Clear Shot at Primary Aim: Susceptibility of Trypanosoma cruzi Organelles, Structures and Molecular Targets to Drug Treatment. Curr Top Med Chem. 2017;17(10):1212-1234. doi: 10.2174/1568026616666161025161858. PMID: 27784255.
16: Salomao K, Menna-Barreto RF, de Castro SL. Stairway to Heaven or Hell? Perspectives and Limitations of Chagas Disease Chemotherapy. Curr Top Med Chem. 2016;16(20):2266-89. doi: 10.2174/1568026616666160413125049. PMID: 27072716.
17: Wanjek M, Senner V, Scharhag-Rosenberger F, Halle M. Effects of different weight loss intervention programmes in health clubs - an observational multicenter study. Eur J Sport Sci. 2016 Oct;16(7):859-67. doi: 10.1080/17461391.2016.1139628. Epub 2016 Feb 2. PMID: 26835870.
18: Asada M. [Development and Distribution of Drugs for NTDs: Efforts of One Pharmaceutical Company]. Yakugaku Zasshi. 2016;136(2):223-30. Japanese. doi: 10.1248/yakushi.15-00233-3. PMID: 26831797.
19: Gaspar L, Moraes CB, Freitas-Junior LH, Ferrari S, Costantino L, Costi MP, Coron RP, Smith TK, Siqueira-Neto JL, McKerrow JH, Cordeiro-da-Silva A. Current and Future Chemotherapy for Chagas Disease. Curr Med Chem. 2015;22(37):4293-312. doi: 10.2174/0929867322666151015120804. PMID: 26477622.
20: Lee TE, Black SA, Fellous A, Yamaguchi N, Angelici FM, Al Hikmani H, Reed JM, Elphick CS, Roberts DL. Assessing uncertainty in sighting records: an example of the Barbary lion. PeerJ. 2015 Sep 1;3:e1224. doi: 10.7717/peerj.1224. PMID: 26357597; PMCID: PMC4562256.
