Selective inhibitor of the mitochondrial Na + -Ca 2+ exchanger (IC 50 = 0.4 μM).
Specific inhibitor of mitochondrial Na+/Ca2+ exchange as well as sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels.
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of Sodium/potassium/calcium exchanger 6
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
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.
Product description
CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
Associated Targets(Human)
SLC8B1TbioMitochondrial sodium/calcium exchanger protein (0 Activities)
1.Ruiz A, Alberdi E, Matute C. (2014) CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels.. Cell Death Dis, 5 (13):(e1156). [PMID:24722281][10.1021/op500134e]
2.Martínez-Sanz FJ, Lajarín-Cuesta R, González-Lafuente L, Moreno-Ortega AJ, Punzón E, Cano-Abad MF, de los Ríos C. (2016) Neuroprotective profile of pyridothiazepines with blocking activity of the mitochondrial Na(+)/Ca(2+) exchanger.. Eur J Med Chem, 109 (13):(114-23). [PMID:26774037][10.1021/op500134e]
3.Bondarenko AI et al.. (2013) Characterization of distinct single-channel properties of Ca(2+) inward currents in mitochondria.. Pflugers Arch, [PMID:23397170]
4.Parnis J et al.. (2013) Mitochondrial exchanger NCLX plays a major role in the intracellular Ca2+ signaling, gliotransmission, and proliferation of astrocytes.. J Neurosci, 33 (17):(7206-19). [PMID:23616530]
5.Jean-Quartier C et al.. (2012) Studying mitochondrial Ca(2+) uptake - a revisit.. Mol Cell Endocrinol, 353 (1-2):(114-27). [PMID:22100614]
6.Agarwal A et al.. (2017) Transient Opening of the Mitochondrial Permeability\xa0Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes.. Neuron, 93 (3):(587-605.e7). [PMID:28132831]
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C2329905