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CGP37157

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Chemical Structure| 75450-34-9 同义名 : -
CAS号 : 75450-34-9
货号 : A510124
分子式 : C15H11Cl2NOS
纯度 : 98%
分子量 : 324.225
MDL号 : MFCD09055422
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(370.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 CGP37157 is identified as a potent and selective inhibitor of the Na+/Ca2+ exchanger, particularly effective in blocking Na+-induced Ca2+-release from guinea-pig heart mitochondria at an IC50 of 0.8 μM. At a concentration of 10 μM, CGP37157 inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, managing intracellular Ca2+ levels by dampening voltage-gated calcium channels and mitigating NMDA-induced rises in cytosolic and mitochondrial Ca2+. Additionally, CGP37157 at this concentration diminishes NMDA-triggered excitotoxicity through the reduction of mitochondrial damage and calpain activity in neurons[2]. CGP37157 (10 μM) combined with salomycin significantly decreased the viability of FaDu and HLaC79 cells, and increased cell apoptosis. In addition, CGP37157 had no inhibitory effect on the tumor toxicity of salomycin [3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.42mL

3.08mL

1.54mL

30.84mL

6.17mL

3.08mL
参考文献

[1]Chiesi M, et al. Structural dependency of the inhibitory action of benzodiazepines and related compounds on the mitochondrial Na+-Ca2+ exchanger. Biochem Pharmacol. 1988 Nov 15;37(22):4399-403.

[2]Ruiz A, et al. CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels. Cell Death Dis. 2014 Apr 10;5:e1156.

[3]Scherzed A, et al. Effects of salinomycin and CGP37157 on head and neck squamous cell carcinoma cell lines in vitro. Mol Med Rep. 2015 Sep;12(3):4455-61.