1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Ferroptosis Reactive Oxygen Species (ROS) Keap1-Nrf2
  3. Ferroptosis-IN-24

Ferroptosis-IN-24 是一种能透过血脑屏障的非经典铁死亡 (ferroptosis) 抑制剂,对 RSL3 (HY-100218A) 和 Erastin (HY-15763) 诱导的铁死亡具有纳摩尔级抑制活性。Ferroptosis-IN-24 可缓解氧化应激,减少脂质过氧化积累,恢复氧化还原稳态。Ferroptosis-IN-24 可用于脑缺血再灌注损伤及急性肝损伤的相关研究。

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Ferroptosis-IN-24

Ferroptosis-IN-24 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ferroptosis-IN-24 is a non-classical ferroptosis inhibitor capable of crossing the blood-brain barrier, with nanomolar inhibitory activity against ferroptosis induced by RSL3 (HY-100218A) and Erastin (HY-15763). Ferroptosis-IN-24 alleviates oxidative stress, reduces lipid peroxidation accumulation, and restores redox homeostasis. Ferroptosis-IN-24 is applicable to research related to cerebral ischemia-reperfusion injury and acute liver injury[1].

体外研究
(In Vitro)

Ferroptosis-IN-24 (compound D12) (6.25-12.5 μM; 24 h) 可强效抑制 PC12 细胞中 RSL3 (HY-100218A) 诱导的铁死亡,其 EC50 为 39.7 nM;在 6.25 μM 和 12.5 μM 浓度下,分别可将细胞存活率提升至 90.7% 和 96.5%[1]
Ferroptosis-IN-24 (24 h) 可抑制 Erastin (HY-15763) 诱导的 PC12 细胞铁死亡,其 EC50 为 410.4 nM[1]
Ferroptosis-IN-24 (1 μM; 8 h) 可有效降低 PC12 细胞中 RSL3 诱导的细胞内 ROS 积累[1]
Ferroptosis-IN-24 (1 μM; 8 h) 可有效抑制 PC12 细胞中由 RSL3 诱导的脂质过氧化[1]
Ferroptosis-IN-24 (1 μM; 6 h) 可逆转 RSL3 诱导的 PC12 细胞中 GPX4 和 Nrf2 蛋白表达下调[1]
Ferroptosis-IN-24 (1 μM) 可降低 RSL3 处理的 PC12 细胞中应激诱导的 GPX4、Nrf2、HMOX1 和 NQO1 mRNA 过表达,表明它缓解的是上游氧化应激而非直接激活 Nrf2 通路[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PC12 cells (RSL3-induced ferroptosis)
Concentration: 6.25 μM; 12.5 μM
Incubation Time: 24 h
Result: Increased PC12 cell viability to 90.7% under RSL3-induced ferroptosis conditions at 6.25 μM.
Increased cell viability to 96.5% under RSL3-induced ferroptosis conditions at 12.5 μM.

Western Blot Analysis[1]

Cell Line: PC12 cells (RSL3-treated)
Concentration: 1 μM
Incubation Time: 6 h
Result: Reversed the RSL3-induced downregulation of GPX4 protein levels in PC12 cells, restoring expression to near-control levels.
Reversed the RSL3-induced downregulation of Nrf2 protein levels in PC12 cells, restoring expression to near-control levels.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUC0-∞ T1/2 V CL AUC0-t
Rat[1] 10 mg/kg i.v. 8199.91 μg/L 0.08 h 4208.09 μg/L·h 4.76 h 0.53 L/kg 2.38 L/h/kg 3350.27 μg/L·h
体内研究
(In Vivo)

Ferroptosis-IN-24 (10-20 mg/kg;腹腔注射;单次预处理) 可在对乙酰氨基酚诱导的急性肝损伤小鼠模型中剂量依赖性地减轻肝坏死、恢复肝酶和抗氧化剂水平,并改善组织学表现[1]
Ferroptosis-IN-24 (10 mg/kg;静脉注射;单次预处理) 可减轻 MCAO 诱导的大鼠脑缺血再灌注损伤模型的脑梗死体积并改善神经功能缺损[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, APAP-induced acute liver injury model)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; single pretreatment (1 h before APAP challenge)
Result: Reduced liver necrosis dose-dependently, with near-normal liver histology at 20 mg/kg.
Reduced serum alanine transaminase (ALT) level and aspartate transaminase (AST) level.
Restored hepatic glutathione (GSH) level.
Reduced malondialdehyde (MDA) level.
Animal Model: SD (male, MCAO-induced cerebral ischemia-reperfusion injury model)[1]
Dosage: 10 mg/kg
Administration: i.v.; single pretreatment (1 h before MCAO, followed by 24 h reperfusion)
Result: Reduced cerebral infarct volume.
Improved neurological deficits.
分子量

293.32

Formula

C18H15NO3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Ferroptosis-IN-24
目录号:
HY-182390
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