7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE Chemical Properties

Boiling point:

479.8±45.0 °C(Predicted)

Density 

1.384±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: ≥20mg/mL

form 

White solid

pka

12.20±0.40(Predicted)

color 

white

Stability:

Stable for 2 years from date of purchase as supplied. Solution in DMSO may be stored at -20°C for up to 3 months.

Safety Information

Hazard Codes 

Xn,N

Risk Statements 

22-50

Safety Statements 

61

WGK Germany 

3

7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE Usage And Synthesis

Description

CGP-37157 (75450-34-9) inhibits?the mitochondrial Na+-Ca2+?exchanger (NCX) in isolated heart mitochondria, IC50=0.36 μM.1?Does not inhibit the plasmalemmal NCX.2? Also inhibits voltage-gated Ca2+?channels in intact cells and therefore its use in cellular studies must employ adequate controls.3? Prevents sudden death in a Guinea pig model of heart failure.4?Displays pronounced cytoprotective effects in chromaffin cells5?and in neuronal injury models.6?Blood-brain barrier permeant.

Uses

7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one is a specific inhibitor of the mitochondrial Na+/Ca2+ exchanger.

Uses

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.

Definition

ChEBI: 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2-one is a benzothiazepine.

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.

Biological Activity

Selective antagonist of the mitochondrial Na + -Ca 2+ exchanger (IC 50 = 0.4 μ M).

Biochem/physiol Actions

Specific inhibitor of mitochondrial Na+/Ca2+ exchange as well as sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels.

storage

Room temperature

References

1) Cox?et al.?(1993),?Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157; J. Cardiovasc. Pharmacol.,?21?595 2) Namekata?et al. (2015),?Pharmacological discrimination of plasmalemmal and mitochondrial sodium-calcium exchanger in cardiomyocyte-derived H9c2 cells; Biol. Pharm. Bull,?38?147 3) Baron & Thayer (1997),?CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons; Eur. J. Pharmacol.,?340?295 4) Liu?et al.?(2014),?Inhibiting mitochondrial Na+/Ca2+ exchange prevents sudden death in a guinea pig model of heart failure; Circ. Res.,?115?44 5) Nicolau?et al.?(2009),?Mitochondrial Na+/Ca2+-exchanger blocker CGP37157 protects against chromaffin cell death elicited by veratridine;?J. Pharmacol. Exp. Ther.,?330?844 6) Ruiz?et al. (2014),?CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage gated Ca2+ channels; Cell Death Dis.,?5?e1156

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