Liproxstatin-1 - Ferroptosis 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELiproxstatin-1Cat. No.: HY-12726CAS No.: 950455-15-9分式: CHClN分量: 340.85作靶点: Ferroptosis作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 31 mg/mL (90.95 mM)* means soluble, but

2、saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9338 mL 14.6692 mL 29.3384 mL5 mM 0.5868 mL 2.9338 mL 5.8677 mL10 mM 0.2934 mL 1.4669 mL 2.9338 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液

3、可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.33 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.33 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molec

4、ules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.33 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Liproxstatin-1种有效的 ferroptosis 抑制剂，IC50 值约为 38 nM。IC50 & Target EC50: 38 nM (ferroptosis) 2体外研究 Liproxstatin-1 prevents BODIPY 581/591 C11 oxidation in Gpx4/ cells. Moreover, Liproxstatin-1 does notinterfer

5、e with other classical types of cell death, such as TNF-induced apoptosis and H2O2-inducednecrosis, and in the bona fide L929 model of TNF/zvad-induced necroptosis 1. Liproxstatin-1 has greatantiferroptotic activity with EC50 of appr 38 nM. Fer-1 and Liproxstatin-1 are inherently good, but not great

6、,radical-trapping antioxidants, but they are excellent in phospholipid bilayers. Fer-1 (10 M) and Liproxstatin-1(10 M) do not exhibit significant inhibitory activity in the 15-LOX-1 overexpressing cells, and theconcentration is almost 1000-fold higher than their EC50s for subverting RSL3-induced fer

7、roptosis in thesecells (15 and 27 nM, respectively) 2.体内研究 Liproxstatin-1 (10 mg/kg, i.p.) suppresses ferroptosis in human cells, Gpx4/ kidney and in anischaemia/reperfusion-induced tissue injury model 1.PROTOCOLCell Assay 1 To induce the knockout of Gpx4, cells are seeded onto 96-well plates (1,000

8、 cells per well) and treated with 1M 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, celldeath is also quantified by measuring released lact

9、ate dehydrogenase (LDH) activity using the CytotoxicityDetection Kit.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Animals includes in the treatment study of inducible Gpx4/ mice are equally distributed between sex andAdministration 1 weight, w

10、ith 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 isarranged to have a similar distribution between females and males. For the pharmacological inhibitorexperiments,

11、 CreERT2;Gpx4fl/fl mice are injected on day 1 and 3 with 0.5 mg TAM dissolved in Miglyol. Onday 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

12、. Survival analysis is performed using the GraphPad Prism software and statistical analysis is doneaccording to the log-rank test.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Redox Biol. 20

13、19 Jun;24:101211. Biomater Sci. 2019 Mar 26;7(4):1311-1322. Oncol Rep. 2019 Jun 6. Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303. J Inflamm. 2019 May.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Friedmann Angeli JP, et al. Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice. Nat Cell Biol. 2014Dec;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 FerroptoticCell Death. ACS Cent Sci. 2017 Mar 22;3(3):