C8874

CGP-37157

Name: CGP-37157
Brand: SIGMA
Price: 3980 CZK

≥98% (HPLC), SERCA antagonist , powder

Synonym(s):

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

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5 MG

CZK 3,980.00

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CZK 13,430.00

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₁₁Cl₂NOS

CAS Number:

75450-34-9

Molecular Weight:

324.22

UNSPSC Code:

12352200

PubChem Substance ID:

329775189

NACRES:

NA.25

MDL number:

MFCD09055422

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Key Documents

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Product Name

CGP-37157, ≥98% (HPLC), powder

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

assay

≥98% (HPLC)

form

powder

color

white

solubility

DMSO: ≥20 mg/mL

storage temp.

2-8°C

Quality Level

100

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Show Differences

1 of 4

This Item	SML2761	SML2760	C5174
Sigma-Aldrich C8874 CGP-37157	Sigma-Aldrich SML2761 SGC6870N	Sigma-Aldrich SML2760 SGC6870	Sigma-Aldrich C5174 4′-Chlorodiazepam
form powder	form powder	form powder	form powder
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (TLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 200
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. -
solubility DMSO: ≥20 mg/mL	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 2 mg/mL, clear	solubility 2-hydroxypropyl-β-cyclodextrin: insoluble, H₂O: insoluble
color white	color white to beige	color white to beige	color -

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.[1]

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

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WGK 3

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Cyclophilin D regulates neuronal activity-induced filopodiagenesis by fine-tuning dendritic mitochondrial calcium dynamics

Sui S, et al.

Journal of Neurochemistry (2018)

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)

Depolarization-induced calcium responses in sympathetic neurons: relative contributions from Ca2+ entry, extrusion, ER/mitochondrial Ca2+ uptake and release, and Ca2+ buffering.

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

Dissection of mitochondrial Ca2+ uptake and release fluxes in situ after depolarization-evoked [Ca2+](i) elevations in sympathetic neurons.

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+

CGP-37157 inhibits the sarcoplasmic reticulum Ca²+ ATPase and activates ryanodine receptor channels in striated muscle.

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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CGP-37157