Synonym
Ferrostatin-1; Frer-1;
IUPAC/Chemical Name
3-amino-4-(cyclohexylamino)-benzoic acid, ethyl ester
InChi Key
UJHBVMHOBZBWMX-UHFFFAOYSA-N
InChi Code
UJHBVMHOBZBWMX-UHFFFAOYSA-N
SMILES Code
O=C(OCC)C1=CC=C(NC2CCCCC2)C(N)=C1
Purity
>98% (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
>2 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
2934.99.9001
Biological target:
Ferrostatin-1, a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM).
In vitro activity:
The expression levels of AT1R, IL-6, IL-1β, COX-2, and GFAP in the astrocytes were significantly elevated by stimulation with Ang II and greatly suppressed by the introduction of Ferrostatin-1 in a dose-dependent manner. The promoted ROS level and inhibited GSH level in the astrocytes by the stimulation with Ang II were significantly reversed by Ferrostatin-1. Down-regulated GPx4, Nrf2, and HO-1 in the astrocytes induced by Ang II were extremely up-regulated by the treatment of Ferrostatin-1 in a dose-dependent manner.
Reference: Int Immunopharmacol. 2021 Jan;90:107179. https://pubmed.ncbi.nlm.nih.gov/33278745/
In vivo activity:
Consistently, the results of in vivo studies demonstrated that ferrostatin-1 protected against light-induced ferroptosis in rats. And it exerted therapeutic effects by inhibiting neuroinflammation and prevented the effects of light exposure on the structure and function of the retina.
Reference: Biochem Biophys Res Commun. 2021 Apr 9;548:27-34. https://pubmed.ncbi.nlm.nih.gov/33631670/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
53.3 |
203.20 |
|
| DMF |
30.0 |
114.35 |
|
| DMF:PBS (pH 7.2) (1:4) |
0.2 |
0.76 |
|
| Ethanol |
29.4 |
112.10 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
262.35
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:
1. Li S, Zhou C, Zhu Y, Chao Z, Sheng Z, Zhang Y, Zhao Y. Ferrostatin-1 alleviates angiotensin II (Ang II)- induced inflammation and ferroptosis in astrocytes. Int Immunopharmacol. 2021 Jan;90:107179. doi: 10.1016/j.intimp.2020.107179. Epub 2020 Dec 2. PMID: 33278745.
2. Anthonymuthu TS, Tyurina YY, Sun WY, Mikulska-Ruminska K, Shrivastava IH, Tyurin VA, Cinemre FB, Dar HH, VanDemark AP, Holman TR, Sadovsky Y, Stockwell BR, He RR, Bahar I, Bayır H, Kagan VE. Resolving the paradox of ferroptotic cell death: Ferrostatin-1 binds to 15LOX/PEBP1 complex, suppresses generation of peroxidized ETE-PE, and protects against ferroptosis. Redox Biol. 2021 Jan;38:101744. doi: 10.1016/j.redox.2020.101744. Epub 2020 Oct 16. PMID: 33126055; PMCID: PMC7596334.
3. Tang W, Guo J, Liu W, Ma J, Xu G. Ferrostatin-1 attenuates ferroptosis and protects the retina against light-induced retinal degeneration. Biochem Biophys Res Commun. 2021 Apr 9;548:27-34. doi: 10.1016/j.bbrc.2021.02.055. Epub 2021 Feb 22. PMID: 33631670.
4. Hu B, Liu Y, Chen X, Zhao J, Han J, Dong H, Zheng Q, Nie G. Ferrostatin-1 protects auditory hair cells from cisplatin-induced ototoxicity in vitro and in vivo. Biochem Biophys Res Commun. 2020 Dec 17;533(4):1442-1448. doi: 10.1016/j.bbrc.2020.10.019. Epub 2020 Oct 24. PMID: 33109343.
In vitro protocol:
1. Li S, Zhou C, Zhu Y, Chao Z, Sheng Z, Zhang Y, Zhao Y. Ferrostatin-1 alleviates angiotensin II (Ang II)- induced inflammation and ferroptosis in astrocytes. Int Immunopharmacol. 2021 Jan;90:107179. doi: 10.1016/j.intimp.2020.107179. Epub 2020 Dec 2. PMID: 33278745.
2. Anthonymuthu TS, Tyurina YY, Sun WY, Mikulska-Ruminska K, Shrivastava IH, Tyurin VA, Cinemre FB, Dar HH, VanDemark AP, Holman TR, Sadovsky Y, Stockwell BR, He RR, Bahar I, Bayır H, Kagan VE. Resolving the paradox of ferroptotic cell death: Ferrostatin-1 binds to 15LOX/PEBP1 complex, suppresses generation of peroxidized ETE-PE, and protects against ferroptosis. Redox Biol. 2021 Jan;38:101744. doi: 10.1016/j.redox.2020.101744. Epub 2020 Oct 16. PMID: 33126055; PMCID: PMC7596334.
In vivo protocol:
1. Tang W, Guo J, Liu W, Ma J, Xu G. Ferrostatin-1 attenuates ferroptosis and protects the retina against light-induced retinal degeneration. Biochem Biophys Res Commun. 2021 Apr 9;548:27-34. doi: 10.1016/j.bbrc.2021.02.055. Epub 2021 Feb 22. PMID: 33631670.
2. Hu B, Liu Y, Chen X, Zhao J, Han J, Dong H, Zheng Q, Nie G. Ferrostatin-1 protects auditory hair cells from cisplatin-induced ototoxicity in vitro and in vivo. Biochem Biophys Res Commun. 2020 Dec 17;533(4):1442-1448. doi: 10.1016/j.bbrc.2020.10.019. Epub 2020 Oct 24. PMID: 33109343.
1: Horwath MC, Bell-Horwath TR, Lescano V, Krishnan K, Merino EJ, Deepe GS Jr.
Antifungal Activity of the Lipophilic Antioxidant Ferrostatin-1. Chembiochem.
2017 Oct 18;18(20):2069-2078. doi: 10.1002/cbic.201700105. Epub 2017 Sep 1.
PubMed PMID: 28783875.
2: Zilka O, Shah R, Li B, Friedmann Angeli JP, Griesser M, Conrad M, Pratt DA. On
the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role
of Lipid Peroxidation in Ferroptotic Cell Death. ACS Cent Sci. 2017 Mar
22;3(3):232-243. doi: 10.1021/acscentsci.7b00028. Epub 2017 Mar 7. PubMed PMID:
28386601; PubMed Central PMCID: PMC5364454.
3: Ito K, Eguchi Y, Imagawa Y, Akai S, Mochizuki H, Tsujimoto Y. MPP+ induces
necrostatin-1- and ferrostatin-1-sensitive necrotic death of neuronal SH-SY5Y
cells. Cell Death Discov. 2017 Feb 27;3:17013. doi: 10.1038/cddiscovery.2017.13.
eCollection 2017. PubMed PMID: 28250973; PubMed Central PMCID: PMC5327502.
4: Kabiraj P, Valenzuela CA, Marin JE, Ramirez DA, Mendez L, Hwang MS,
Varela-Ramirez A, Fenelon K, Narayan M, Skouta R. The neuroprotective role of
ferrostatin-1 under rotenone-induced oxidative stress in dopaminergic
neuroblastoma cells. Protein J. 2015 Oct;34(5):349-58. doi:
10.1007/s10930-015-9629-7. PubMed PMID: 26385697.
