Molecular structure of CGP 37157, CAS Number: 75450-34-9
CGP 37157 (CAS 75450-34-9)
See product citations (3)
Alternate Names:
7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
Application:
CGP 37157 is a benzothiazepine compound that acts as a potent inhibitor of mitochondrial Na+/Ca2+ exchanger
CAS Number:
75450-34-9
Purity:
98%
Molecular Weight:
324.20
Molecular Formula:
C15H11Cl2NOS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
CGP 37157 is a benzothiazepine compound that is derived from clonazepam and described to act as a selective and potent inhibitor of mitochondrial NCX (Na+/Ca2+ exchanger). Studies report that CGP 37157 inhibits voltage-gated Ca2+ channels directly and the mitochondrial Ca2+ efflux. CGP 37157 may act to activate ryanodine receptors channels and inhibit SERCA (sarcoplasmic reticulum Ca2+ ATPase) in striated muscle. Additionally, studies reveal that inhibition of the mitochondrial NCX (Na+/Ca2+ exchanger) by CGP 37157 elevates insulin secretion and ATP synthesis in rat islets.
CGP 37157 (CAS 75450-34-9) References
- Pharmacological investigation of mitochondrial ca(2+) transport in central neurons: studies with CGP-37157, an inhibitor of the mitochondrial Na(+)-Ca(2+) exchanger. | Scanlon, JM., et al. 2000. Cell Calcium. 28: 317-27. PMID: 11115371
- Inhibition of canine (NCX1.1) and Drosophila (CALX1.1) Na(+)-Ca(2+) exchangers by 7-chloro-3,5-dihydro-5-phenyl-1H-4,1-benzothiazepine-2-one (CGP-37157). | Omelchenko, A., et al. 2003. J Pharmacol Exp Ther. 306: 1050-7. PMID: 12808003
- Inhibition of plasmalemmal Na(+)/Ca(2+) exchange by mitochondrial Na(+)/Ca(2+) exchange inhibitor 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one (CGP-37157) in cerebellar granule cells. | Czyz, A. and Kiedrowski, L. 2003. Biochem Pharmacol. 66: 2409-11. PMID: 14637198
- Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes. | Thu, le T., et al. 2006. Eur J Pharmacol. 552: 15-9. PMID: 17054940
- Voltage-gated Ca(2+) influx and insulin secretion in human and mouse beta-cells are impaired by the mitochondrial Na(+)/Ca(2+) exchange inhibitor CGP-37157. | Luciani, DS., et al. 2007. Eur J Pharmacol. 576: 18-25. PMID: 17719029
- Inhibition of mitochondrial calcium uptake rather than efflux impedes calcium release by inositol-1,4,5-trisphosphate-sensitive receptors. | Chalmers, S. and McCarron, JG. 2009. Cell Calcium. 46: 107-13. PMID: 19577805
- CGP-37157 inhibits the sarcoplasmic reticulum Ca²+ ATPase and activates ryanodine receptor channels in striated muscle. | Neumann, JT., et al. 2011. Mol Pharmacol. 79: 141-7. PMID: 20923851
- Pharmacological discrimination of plasmalemmal and mitochondrial sodium-calcium exchanger in cardiomyocyte-derived H9c2 cells. | Namekata, I., et al. 2015. Biol Pharm Bull. 38: 147-50. PMID: 25744471
- Targeting Mitochondrial Calcium Handling and Reactive Oxygen Species in Heart Failure. | Dietl, A. and Maack, C. 2017. Curr Heart Fail Rep. 14: 338-349. PMID: 28656516
- Pharmacologic inhibition of the mitochondrial Na+/Ca2+ exchanger protects against ventricular arrhythmias in a porcine model of ischemia-reperfusion. | Sventzouri, S., et al. 2018. Hellenic J Cardiol. 59: 217-222. PMID: 29292245
- Pharmacological Comparisons Between Cannabidiol and KLS-13019. | Brenneman, DE., et al. 2018. J Mol Neurosci. 66: 121-134. PMID: 30109468
- Impact of mitochondria on local calcium release in murine sinoatrial nodal cells. | Takeda, Y. and Matsuoka, S. 2022. J Mol Cell Cardiol. 164: 42-50. PMID: 34826768
- Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157. | Cox, DA., et al. 1993. J Cardiovasc Pharmacol. 21: 595-9. PMID: 7681905
- Inhibition of mitochondrial calcium efflux by clonazepam in intact single rat cardiomyocytes and effects on NADH production. | Griffiths, EJ., et al. 1997. Cell Calcium. 21: 321-9. PMID: 9160168
- CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons. | Baron, KT. and Thayer, SA. 1997. Eur J Pharmacol. 340: 295-300. PMID: 9537826
Inhibitor of:
β′-COP, BSPII, C8β, CBARA1 (MICU1), CCDC109A, CCDC109B, CCDC90A, connexin 33, hippocalcin, Na+/K+-ATPase β3, NCX, NCX2, Olfr370, Olfr936, PMCA2, RyR-1, SERCA, SERCA2, SLN, smoothelin, and Tom40B.Activator of:
ATPAF1, CaBP5, CALHM2, Gm5849, Junctional SR Marker, Junctophilin-1, KCNMB3, NCX1, NCX3, phospholamban, and Tom70.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CGP 37157, 5 mg | sc-202097 | 5 mg | $113.00 | |||
CGP 37157, 25 mg | sc-202097A | 25 mg | $454.00 |