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C8874

Sigma-Aldrich

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:
75450-34-9
Molecular Weight:
324.22
MDL number:
MFCD09055422
UNSPSC Code:
12352200
PubChem Substance ID:
329775189
NACRES:
NA.25

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

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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
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
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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