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| | 7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE Basic information |
| Product Name: | 7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE | | Synonyms: | 7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE;CGP 37157;7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one;4,1-Benzothiazepin-2(3H)-one, 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-;7-chloro-5-(2-chlorophenyl)benzo[e][1,4]thiazepin-2(1H,3H,5H)-one;CGP-37157 - CAS 75450-34-9 - Calbiochem;1-benzothiazepine-2(3H)-one;7-Chloro-5-(2-chlorophenyl)-1 | | CAS: | 75450-34-9 | | MF: | C15H11Cl2NOS | | MW: | 324.22 | | EINECS: | | | Product Categories: | Ion transporter and other ion channel;Signalling | | Mol File: | 75450-34-9.mol |  |
| | 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 | | pka | 12.20±0.40(Predicted) | | form | White solid | | 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. |
| 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 |
| | 7-CHLORO-5-(2-CHLOROPHENYL)-1,5-DIHYDRO-4,1-BENZOTHIAZEPIN-2(3H)-ONE Preparation Products And Raw materials |
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