生物活性
Ferrostatin-1 (Fer-1)是一种有效的选择性的ferroptosis抑制剂,抑制Erastin诱导的HT-1080细胞铁死亡,EC50为60 nM。Ferrostatin-1(2 μM)作用于癌细胞,抑制Erastin诱导的Ferroptosis,Ferroptosis是一种铁依赖性的的非凋亡性细胞死亡,Ferrostatin-1作用于新生大鼠脑片,抑制 谷氨酸盐诱导的细胞死亡。Ferrostatin-1是一种脂质ROS清除剂,具有N-环己基部分,作为生物膜内亲脂锚。Ferrostatin-1还是一种抗氧化剂,通过还原机制来防止膜脂的损伤,从而抑制细胞死亡。Ferrostatin-1也具有抗真菌活性。
化学数据
分子量 | 262.35 |
分子式 | C15H22N2O2 |
CAS号 | 347174-05-4 |
纯度 | 98.43% |
溶解性(25°C) | DMSO 40 mg/mL |
储存和运输条件 | -20°C, protect from light, dry, sealed 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | BEAS-2B cells |
方法 | Cell viability assay In brief, BEAS-2B cells were seeded into a 96-well plate at the concentration of 5 × 104cells/well. The cells were cultured for 24 h, then treated with LPS (Sigma) and Fer-1 (Sigma) in different concentrations for 16 h followed by the addition of 20 μl of CCK-8 solution directly into the medium (200 μl per well) and incubation at 37 °C for 4 h. The absorbances (Abs) in different groups were detected at 450 nm (n = 3). In the blank group, the well only contained medium, and the cells without any treatment were used as the control group. Herein, the cell viability = (Abs of experimental group-Abs of blank group)/(Abs of control group-Abs of blank group) × 100%. |
浓度 | 2 μM |
处理时间 | 16 h |
动物实验 |
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动物模型 | male C57BL/6 mice |
配制 | The Fer-1 was dissolved in DMSO first, and diluted with 0.9% NaCl. The final concentration of Fer-1 and DMSO was 0.2 mg/ml and 0.1% respectively. |
剂量 | 0.8 mg/kg |
给药处理 | via tail vein injection |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 3.8117 mL | 19.0585 mL | 38.117 mL |
5 mM | 0.7623 mL | 3.8117 mL | 7.6234 mL |
10 mM | 0.3812 mL | 1.9059 mL | 3.8117 mL |