CGP37157

产品编号 T14941Cas号 75450-34-9

别名 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one

CGP37157 (7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one) 是一种 Na+/Ca2+ 交换抑制剂，抑制 Na+ 诱导的豚鼠心脏线粒体中 Ca2+ 的释放，IC50 为 0.8 μM。

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产品编号 T14941别名 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-oneCas号 75450-34-9

CGP37157 (7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one) 是一种 Na+/Ca2+ 交换抑制剂，抑制 Na+ 诱导的豚鼠心脏线粒体中 Ca2+ 的释放，IC50 为 0.8 μM。

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生物活性

产品描述	CGP37157 (7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one) is a Na+/Ca2+ exchanger inhibitor, inhibits Na+-induced Ca2+ release from mitochondria in guinea pig heart with IC50 of 0.8 μM.
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].
别名	7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 65 mg/mL (200.48 mM)

溶液配制表

DMSO