Ferrostatin-1 (Fer-1)

Alias: Frer-1; 3-amino-4-(cyclohexylamino)-benzoic acid, ethyl ester; Ferrostatin-1;
Cat No.:V0955 Purity: ≥98%
Ferrostatin-1 (also named as Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Ferrostatin-1 (Fer-1) Chemical Structure CAS No.: 347174-05-4
Product category: Ferroptosis
This product is for research use only, not for human use. We do not sell to patients.
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InvivoChem's Ferrostatin-1 (Fer-1) has been cited by 2 publications
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Ferrostatin-1 (also named as Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. It is the most potent inhibitor of erastin-induced ferroptosis in HT-1080 cells (EC50 of 60 nM). Ferrostatin-1 does not inhibit ERK phosphorylation or arrest the proliferation of HT-1080 cells. Ferroptosis is a regulated, oxidative, nanapoptotic cell death, Ferrostatin-1 has been founded as a potent inhibitor of it. Ferrostatin-1 can attenuate oxidative, iron-dependent cancer cell death through blocking cystine import and glutathione production. It had been reported to prevent Huntington's disease cellular models to death by inhibiting lipid peroxidation.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ferrostatin-1 inhibits the build-up of lipid and cytosolic ROS that is generated by erastin. Neurotoxicity caused by glutamate is inhibited in organotypic rat brain slices by ferrostatin-1 [1]. Rat organotypic hippocampal slice cultures (OHSC) are protected from glutamate (5 mM)-induced neurotoxicity by ferrostatin-1 (2 μM; 24 hours) [2]. Ferrostatin-1 suppresses lipid peroxidation, but not the permeability of lysosomal membranes or the production of reactive oxygen species in the mitochondria [2]. In cellular models of renal failure, periventricular leukomalacia (PVL), and Huntington's disease (HD), ferrostatin-1 reduces cell death [2]. In HT-1080 cells, ferrostatin-1 (1 μM; 6 hours) prevents unsaturated fatty acid oxidative degradation, which increases the quantity of healthy medium spiny neurons (MSNs) [3].
ln Vivo
In mice with rhabdomyolysis, ferrostatin-1 (5 mg/kg; i.p.; single dosage, given 30 min before glycerol injection) improves renal function; however, this benefit is not shown in mice lacking in the pan-caspase inhibitor zVAD or RIPK3. Acute lung damage (ALI) caused by LPS can be efficiently treated with ferrostatin-1 (0.8 mg/kg; tail vein injection)[4]. Rhabdomyolysis-affected mice's renal function is improved by ferrostatin-1 (5 mg/kg; i.p.; C57BL/6J mice) [5].
Animal Protocol
Animal/Disease Models: Male C57BL/6 mice (LPS-induced ALI)[4]
Doses: 0.8 mg/kg
Route of Administration: Tail vein injection
Experimental Results: Exerted therapeutic action against LPS-induced ALI.
References
[1]. Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012;149(5):1060-1072.
[2]. Skouta R, Dixon SJ, Wang J, et al. Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models. J Am Chem Soc. 2014;136(12):4551-4556.
[3]. Horwath MC, et al. Antifungal Activity of the Lipophilic Antioxidant Ferrostatin-1. Chembiochem. 2017;18(20):2069-2078.
[4]. Liu P, Feng Y, et al. Ferrostatin-1 alleviates lipopolysaccharide-induced acute lung injury via inhibiting ferroptosis. Cell Mol Biol Lett. 2020;25:10. Published 2020 Feb 27.
[5]. Melania Guerrero Hue, et al. FP282 FERROPTOSIS-MEDIATED CELL DEATH IS DECREASED BY CURCUMIN IN RENAL DAMAGE ASSOCIATED TO RHABDOMYOLYSIS, Nephrology Dialysis Transplantation, Volume 34, Issue Supplement_1, June 2019, gfz106.FP282.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H22N2O2
Molecular Weight
262.35
CAS #
347174-05-4
SMILES
O=C(OCC)C1=CC=C(NC2CCCCC2)C(N)=C1
Chemical Name
3-amino-4-(cyclohexylamino)-benzoic acid, ethyl ester
Synonyms
Frer-1; 3-amino-4-(cyclohexylamino)-benzoic acid, ethyl ester; Ferrostatin-1;
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 Data
Solubility (In Vitro)
DMSO: 52 mg/mL (198.2 mM)
Water:<1 mg/mL
Ethanol:52 mg/mL (198.2 mM)
Solubility (In Vivo)
2% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.8117 mL 19.0585 mL 38.1170 mL
5 mM 0.7623 mL 3.8117 mL 7.6234 mL
10 mM 0.3812 mL 1.9059 mL 3.8117 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.

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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.

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Biological Data
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