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CGP37157

CAS号

75450-34-9

分子式

C15H11Cl2NOS

主要靶点

Na+/Ca2+ Exchanger

仅限科研使用

Cat No : CM07517

Print datasheet

Synonyms

Ca2+ Exchanger|Ca2+Exchanger|CGP37157|CGP-37157|CGP 37157|7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one|Inhibitor|inhibit|Na+Exchanger|Na+/Ca2+ exchanger|Na+/Ca2+ Exchanger|Na+ Exchanger

验证数据展示

  • CAS No.: 75450-34-9

    CGP37157
    CAS#: 75450-34-9

产品信息

CAS号 75450-34-9
分子式 C15H11Cl2NOS
主要靶点 Na+/Ca2+ Exchanger
主要通路 离子通道
分子量 324.22
纯度 99.04%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Ca2+ Exchanger|Ca2+Exchanger|CGP37157|CGP-37157|CGP 37157|7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one|Inhibitor|inhibit|Na+Exchanger|Na+/Ca2+ exchanger|Na+/Ca2+ Exchanger|Na+ Exchanger

靶点活性

Na+, Ca2+ exchanger:0.8 μM

体外活性

Administration of 10?μM CGP37157 shows an inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulating intracellular Ca2+ levels via suppressing voltage-gated calcium channels. Administration of 10?μM CGP37157 in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. CGP37157 has no inhibitory effect on salinomycin tumor toxicity[2]. Administration of 10?μM CGP37157 reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads and it also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons[3].

溶解度

DMSO:65 mg/mL (200.48 mM)

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.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.
3.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.

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