Home >> Research Area >>Metabolism>>Ferroptosis>> Liproxstatin-1

Liproxstatin-1

A potent ferroptosis inhibitor CAS# 950455-15-9

Liproxstatin-1

Catalog No. BCC5651----Order now to get a substantial discount!

Product Name & Size Price Stock
Liproxstatin-1: 5mg $115 In Stock
Liproxstatin-1: 10mg Please Inquire In Stock
Liproxstatin-1: 20mg Please Inquire Please Inquire
Liproxstatin-1: 50mg Please Inquire Please Inquire
Liproxstatin-1: 100mg Please Inquire Please Inquire
Liproxstatin-1: 200mg Please Inquire Please Inquire
Liproxstatin-1: 500mg Please Inquire Please Inquire
Liproxstatin-1: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Liproxstatin-1

Number of papers citing our products

Chemical structure

Liproxstatin-1

3D structure

Chemical Properties of Liproxstatin-1

Cas No. 950455-15-9 SDF Download SDF
PubChem ID 20931416 Appearance Powder
Formula C19H21ClN4 M.Wt 340.85
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 31 mg/mL (90.95 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[(3-chlorophenyl)methyl]spiro[4H-quinoxaline-3,4'-piperidine]-2-amine
SMILES C1CNCCC12C(=NC3=CC=CC=C3N2)NCC4=CC(=CC=C4)Cl
Standard InChIKey YAFQFNOUYXZVPZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H21ClN4/c20-15-5-3-4-14(12-15)13-22-18-19(8-10-21-11-9-19)24-17-7-2-1-6-16(17)23-18/h1-7,12,21,24H,8-11,13H2,(H,22,23)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Liproxstatin-1

DescriptionLiproxstatin-1 is a potent ferroptosis inhibitor, with IC50 of appr 38 nM.In Vitro:Liproxstatin-1 prevents BODIPY 581/591 C11 oxidation in Gpx4−/− cells. Moreover, Liproxstatin-1 does not interfere with other classical types of cell death, such as TNFα-induced apoptosis and H2O2-induced necrosis, and in the bona fide L929 model of TNFα/zvad-induced necroptosis[1]. Liproxstatin-1 has great antiferroptotic activity with EC50 of appr 38 nM. Fer-1 and Liproxstatin-1 are inherently good, but not great, radical-trapping antioxidants, but they are excellent in phospholipid bilayers. Fer-1 (10 μM) and Liproxstatin-1 (10 μM) do not exhibit significant inhibitory activity in the 15-LOX-1 overexpressing cells, and the concentration is almost 1000-fold higher than their EC50s for subverting RSL3-induced ferroptosis in these cells (15 and 27 nM, respectively)[2].In Vivo:Liproxstatin-1 (10 mg/kg, i.p.) suppresses ferroptosis in human cells, Gpx4−/− kidney and in an ischaemia/reperfusion-induced tissue injury model[1].

References:
[1]. Friedmann Angeli JP, et al. Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice. Nat Cell Biol. 2014 Dec;16(12):1180-91. [2]. Zilka O, et al. 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.

Protocol

Cell Assay [1]
To induce the knockout of Gpx4, cells are seeded onto 96-well plates (1,000 cells per well) and treated with 1 μM 4-OH-tamoxifen (TAM) after plating. Cell viability is assessed at different time points after treatment (usually 72 h) using AquaBluer, unless stated otherwise, as an indicator of viable cells. Alternatively, cell death is also quantified by measuring released lactate dehydrogenase (LDH) activity using the Cytotoxicity Detection Kit.

Animal Administration [1]
Animals includes in the treatment study of inducible Gpx4−/− mice are equally distributed between sex and weight, with typically 8-10 weeks of age. The average weight within the groups is between 22 and 24 g. Groups are formed to have comparable numbers of females/males of the same age. Animal weight is arranged to have a similar distribution between females and males. For the pharmacological inhibitor experiments, CreERT2;Gpx4fl/fl mice are injected on day 1 and 3 with 0.5 mg TAM dissolved in Miglyol. On day 4, compound treatment is started (Liproxstatin-1: 10 mg/kg) along with vehicle control (1% dimethylsulphoxide (DMSO) in PBS). Liproxstatin-1 and vehicle control are administered once daily by i.p. injection. Survival analysis is performed using the GraphPad Prism software and statistical analysis is done according to the log-rank test.

References:
[1]. Friedmann Angeli JP, et al. Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice. Nat Cell Biol. 2014 Dec;16(12):1180-91. [2]. Zilka O, et al. 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.

Liproxstatin-1 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Liproxstatin-1 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Liproxstatin-1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9338 mL 14.6692 mL 29.3384 mL 58.6768 mL 73.346 mL
5 mM 0.5868 mL 2.9338 mL 5.8677 mL 11.7354 mL 14.6692 mL
10 mM 0.2934 mL 1.4669 mL 2.9338 mL 5.8677 mL 7.3346 mL
50 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.1735 mL 1.4669 mL
100 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.5868 mL 0.7335 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Liproxstatin-1

Liproxstatin-1 is a potent ferroptosis inhibitor.

Featured Products
New Products
 

References on Liproxstatin-1

Theoretical insights into the mechanism of ferroptosis suppression via inactivation of a lipid peroxide radical by liproxstatin-1.[Pubmed:28489094]

Phys Chem Chem Phys. 2017 May 24;19(20):13153-13159.

Ferroptosis is a recently discovered iron-dependent form of non-apoptotic cell death caused by the accumulation of membrane lipid peroxidation products, which is involved in various pathological conditions of the brain, kidney, liver and heart. A potent spiroquinoxalinamine derivative named Liproxstatin-1 is discovered by high-throughput screening, which is able to suppress ferroptosis via lipid peroxide scavenging in vivo. Thus, molecular simulations, density functional theory (DFT) and variational transition-state theory with a small-curvature tunneling (SCT) coefficient are utilized to elucidate the detailed mechanisms of inactivation of a lipid peroxide radical by Liproxstatin-1. H-atom abstracted from Liproxstatin-1 by a CH3OO radical occurs preferentially at the aromatic amine site (1'-NH) under thermodynamic and frontier molecular orbital analysis. The value of a calculated rate constant at 300 K is up to 6.38 x 10(3) M(-1) S(-1), indicating that the quantum tunneling effect is responsible for making a free radical trapping reaction more efficient by Liproxstatin-1. The production of a Liproxstatin-1 radical is easily regenerated to the active reduced form by ubiquinol in the body to avoid secondary damage by free radicals. A benzene ring and the higher HOMO energy are beneficial to enhance the lipid radical scavenging activity based on the structure-activity relationship study. Overall, the present results provide theoretical insights into the exploration of novel ferroptosis inhibitors.

On the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role of Lipid Peroxidation in Ferroptotic Cell Death.[Pubmed:28386601]

ACS Cent Sci. 2017 Mar 22;3(3):232-243.

Ferroptosis is a form of regulated necrosis associated with the iron-dependent accumulation of lipid hydroperoxides that may play a key role in the pathogenesis of degenerative diseases in which lipid peroxidation has been implicated. High-throughput screening efforts have identified ferrostatin-1 (Fer-1) and Liproxstatin-1 (Lip-1) as potent inhibitors of ferroptosis - an activity that has been ascribed to their ability to slow the accumulation of lipid hydroperoxides. Herein we demonstrate that this activity likely derives from their reactivity as radical-trapping antioxidants (RTAs) rather than their potency as inhibitors of lipoxygenases. Although inhibited autoxidations of styrene revealed that Fer-1 and Lip-1 react roughly 10-fold more slowly with peroxyl radicals than reactions of alpha-tocopherol (alpha-TOH), they were significantly more reactive than alpha-TOH in phosphatidylcholine lipid bilayers - consistent with the greater potency of Fer-1 and Lip-1 relative to alpha-TOH as inhibitors of ferroptosis. None of Fer-1, Lip-1, and alpha-TOH inhibited human 15-lipoxygenase-1 (15-LOX-1) overexpressed in HEK-293 cells when assayed at concentrations where they inhibited ferroptosis. These results stand in stark contrast to those obtained with a known 15-LOX-1 inhibitor (PD146176), which was able to inhibit the enzyme at concentrations where it was effective in inhibiting ferroptosis. Given the likelihood that Fer-1 and Lip-1 subvert ferroptosis by inhibiting lipid peroxidation as RTAs, we evaluated the antiferroptotic potential of 1,8-tetrahydronaphthyridinols (hereafter THNs): rationally designed radical-trapping antioxidants of unparalleled reactivity. We show for the first time that the inherent reactivity of the THNs translates to cell culture, where lipophilic THNs were similarly effective to Fer-1 and Lip-1 at subverting ferroptosis induced by either pharmacological or genetic inhibition of the hydroperoxide-detoxifying enzyme Gpx4 in mouse fibroblasts, and glutamate-induced death of mouse hippocampal cells. These results demonstrate that potent RTAs subvert ferroptosis and suggest that lipid peroxidation (autoxidation) may play a central role in the process.

Description

Liproxstatin-1 is a potent ferroptosis inhibitor, with IC50 of approximately 38 nM.

Keywords:

Liproxstatin-1,950455-15-9,Natural Products,Ferroptosis, buy Liproxstatin-1 , Liproxstatin-1 supplier , purchase Liproxstatin-1 , Liproxstatin-1 cost , Liproxstatin-1 manufacturer , order Liproxstatin-1 , high purity Liproxstatin-1

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: