Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC₅₀=22 nM)^[1].

IC50: 22 nM (ferroptosis)^[2]

Liproxstatin-1 shows antiferroptotic activity with an IC₅₀ of approximately 38 nM in mouse embryonic fibroblasts^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Liproxstatin-1 (10 mg/kg, i.p.) suppresses ferroptosis in human cells, Gpx4^−/− kidney and in an ischaemia/reperfusion-induced tissue injury model^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

340.85

C₁₉H₂₁ClN₄

950455-15-9

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 31 mg/mL (90.95 mM)

* “≥” means soluble, but saturation unknown.

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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.33 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.33 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.33 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 4.

  请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

  Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution
• 5.

  请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution
• 6.

  请依序添加每种溶剂： 1% DMSO    99% saline

  Solubility: ≥ 0.5 mg/mL (1.47 mM); Clear solution

• [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

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-ICI 47699 (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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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