C8874
CGP-37157
≥98% (HPLC), powder
Synonym(s):
7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
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About This Item
Empirical Formula (Hill Notation):
C15H11Cl2NOS
CAS Number:
Molecular Weight:
324.22
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.25
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
SMILES string
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
General description
CGP-37157 is a benzothiazepine compound, which is derived from clonazepam. It functions as a sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) antagonist and ryanodine receptor channels (RyR) agonist. CGP-37157 regulates intracellular signaling of calcium in smooth, cardiac and skeletal muscle cells and non-muscle systems.
Application
CGP-37157 has been used as a mitochondrial sodium-calcium exchanger (mNCX) inhibitor to study the role of normal mitochondrial calcium dynamics in sustaining dendritic spinogenesis.
Biochem/physiol Actions
Specific inhibitor of mitochondrial Na+/Ca2+ exchange as well as sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels.
WGK
WGK 3
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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
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)
Cyclophilin D regulates neuronal activity-induced filopodiagenesis by fine-tuning dendritic mitochondrial calcium dynamics
Sui S, et al.
Journal of Neurochemistry (2018)
S L Colegrove et al.
The Journal of general physiology, 115(3), 351-370 (2000-02-29)
We studied how mitochondrial Ca2+ transport influences [Ca2+](i) dynamics in sympathetic neurons. Cells were treated with thapsigargin to inhibit Ca2+ accumulation by SERCA pumps and depolarized to elevate [Ca2+(i); the recovery that followed repolarization was then examined. The total Ca2+
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
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