|N-[(3-氯苯基)甲基]-螺[哌啶-4,2'(1'H)-喹喔啉]-3'-胺|CsnPharm

CAS No.: 950455-15-9

Liproxstatin-1/利普司他丁-1 Catalog No. CSN18628

Synonyms: N/A

Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.

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400-920-2911

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tech@csnpharm.cn

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Ferroptosis is a form of regulated apoptosis related to the iron-dependent accumulation of lipid hydroperoxides. Liproxstatin-1 is a potent inhibitor of ferroptosis with an IC50 value of 22 nM in mouse embryonic fibroblasts (MCFs) with an inducible knockdown of glutathione peroxidase 4 (Gpx4^-/-). Liproxstatin-1 at 50 nM completed inhibited lipid peroxidation in Gpx4^-/- cells assessed by using the redox-sensitive dye BODIPY 581/591 C11. Liproxstatin-1 at 200 nM protects against ferroptosis-inducing agents, such as BSO (10 μM), erastin (1 μM) and RSL3 (0.5 μM) as indicated by the percentage of cell viability, whereas it did not rescue other types of cell death, such as staurosporine and H₂O₂-induced necrosis, and the bona fide L929 model of TNFα/zvad-induced necroptosis. In primary human renal proximal tubule epithelial cells (HRPTEpiCs), the incubation of 100 nM Liproxstatin-1 for 24 hours prevented RSL3 (0.2 μM)-induced cell death. Liproxstatin-1 at the same concentration also inhibited RSL3-induced lipid oxidation in HRPTEpiCs. When mice were injected daily with Liproxstatin-1(10 mg/kg) intraperitoneally until the signs of acute renal failure appeared, the survival rate in Liproxstatin-1-treated group were remarkably extended compared with vehicle-treated mice. A significantly reduced number of TUNEL+ cells were also found in Liproxstatin-1-treated group.
作用机制Liproxstatin-1 is a spiroquinoxalinamine derivative that suppresses ferroptosis via lipid peroxide scavenging in vivo. The benzene ring and higher HOMO energy have beneficial effect on increasing the lipid radical scavenging activity.

动物研究

剂量

Mice: 5 mg/kg, 10 mg/kg^[2] (i.p.); 1 mg/kg^[2] (i.v.);

给药途径

i.p., i.v.

动物药代数据

Animal	Mice^[2]
Dose	1 mg/kg (i.v.) 5 mg/kg (p.o.)
Administration	i.v. p.o.
F	52% (p.o.)
V	849 ml (i.v.)
T_1/2	4.5 h (i.v.)
MRT_inf	4.9 h (i.v.)
T_max	2 h (p.o.)
C_max	0.08 µg/ml (p.o.)
C	0.4 μg/ml (i.v.)
CL_total	66 ml/min/kg (i.v.)
Vss	629 ml (i.v.)

参考文献

[1] Kim SE, Zhang L, et al. Ultrasmall nanoparticles induce ferroptosis in nutrient-deprived cancer cells and suppress tumour growth. Nat Nanotechnol. 2016 Nov;11(11):977-985.
[2] Friedmann Angeli JP, Schneider M, et al. Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice. Nat Cell Biol. 2014 Dec;16(12):1180-91.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9338 mL
- 14.6692 mL
- 29.3384 mL
- 5 mM
- 0.5868 mL
- 2.9338 mL
- 5.8677 mL
- 10 mM
- 0.2934 mL
- 1.4669 mL
- 2.9338 mL

技术信息

CAS号

950455-15-9

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21ClN4

运输

蓝冰

分子量

340.85

别名

N/A

溶解度

DMSO	500.0 mg/mL (1466.9 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	40 mg/mL	suspension

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