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

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

Hazard Codes 

Xn,N

Risk Statements 

22-50

Safety Statements 

61

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H400Very toxic to aquatic life

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

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

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