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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white
溶解性
DMSO: ≥20 mg/mL
储存温度
2-8°C
SMILES字符串
Clc1ccc2NC(=O)CSC(c3ccccc3Cl)c2c1
InChI
1S/C15H11Cl2NOS/c16-9-5-6-13-11(7-9)15(20-8-14(19)18-13)10-3-1-2-4-12(10)17/h1-7,15H,8H2,(H,18,19)
InChI key
KQEPIRKXSUIUTH-UHFFFAOYSA-N
一般描述
CGP-37157 是苯并噻氮平化合物，衍生自氯硝西泮。它可作为肌浆网/内质网 Ca2+ ATPase（SERCA）拮抗剂和兰尼碱受体通道（RyR）激动剂。CGP-37157 调节平滑肌、心脏和骨骼肌细胞以及非肌肉系统中钙的胞内信号传导。
应用
CGP-37157 作为线粒体钠钙交换剂（mNCX）抑制剂，用于研究正常线粒体钙动力学在维持树突棘生成中的作用。
生化/生理作用
线粒体 Na+/Ca2+ 交换以及肌质网钙刺激的 ATPase 和其他钙通道的特异性抑制剂。
WGK
WGK 3
CGP-37157 inhibits the sarcoplasmic reticulum Ca2+ ATPase and activates ryanodine receptor channels in striated muscle
Neumann JT, et al.
Molecular Pharmacology, 79(1), 141-147 (2011)
Michael Patterson et al.
The Journal of general physiology, 129(1), 29-56 (2006-12-28)
Many models have been developed to account for stimulus-evoked [Ca(2+)] responses, but few address how responses elicited in specific cell types are defined by the Ca(2+) transport and buffering systems that operate in the same cells. In this study, we
Cyclophilin D regulates neuronal activity-induced filopodiagenesis by fine-tuning dendritic mitochondrial calcium dynamics
Sui S, et al.
Journal of Neurochemistry (2018)
Jake T Neumann et al.
Molecular pharmacology, 79(1), 141-147 (2010-10-07)
7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one [CGP-37157 (CGP)], a benzothiazepine derivative of clonazepam, is commonly used as a blocker of the mitochondrial Na+/Ca²+ exchanger. However, evidence suggests that CGP could also affect other targets, such as L-type Ca²+ channels and plasmalemma Na+/Ca²+ exchanger. Here, we
Cheng Wei Lu et al.
Neurochemistry international, 140, 104845-104845 (2020-09-11)
Indole-3-carbinol (I3C), found in cruciferous vegetables, has been proposed to exhibit neuroprotective effects. This study aimed to investigate the effect of the I3C derivative [1(4-chloro-3-nitrobenzenesulfonyl)-1H-indol-3-yl]-methanol (CIM), which has superior pharmacokinetic properties to I3C, on glutamate release in rat cerebrocortical nerve
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