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 |
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 |
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
以下数据基于半岛bd体育手机客户端 分子量,对于特殊半岛bd体育手机客户端 ,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 |
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 |