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Submit ReviewCGP 37157
Description: Antagonist of mitochondrial Na+/Ca2+ exchange
Chemical Name: 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
Purity: ≥99% (HPLC)
Biological Activity for CGP 37157
CGP 37157 is a selective antagonist of the mitochondrial Na+/Ca2+ exchanger (NCX; IC50 = 0.4 μM).
Compound Libraries for CGP 37157
CGP 37157 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CGP 37157
| M. Wt | 324.22 |
| Formula | C15H11Cl2NOS |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 75450-34-9 |
| PubChem ID | 2688 |
| InChI Key | KQEPIRKXSUIUTH-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C2NC(=O)CSC(C3=CC=CC=C3Cl)C2=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CGP 37157
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 |
Preparing Stock Solutions for CGP 37157
The following data is based on the product molecular weight 324.22. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.08 mL | 15.42 mL | 30.84 mL |
| 5 mM | 0.62 mL | 3.08 mL | 6.17 mL |
| 10 mM | 0.31 mL | 1.54 mL | 3.08 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets for CGP 37157
References for CGP 37157
References are publications that support the biological activity of the product.
Baron and Thayer (1997) CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons. Eur.J.Pharmacol. 340 295 PMID: 9537826
Cox et al (1993) Selectivity of inhibition of Na+-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157. J.Cardiovasc.Pharmacol. 21 595 PMID: 7681905
Cox and Matlib (1993) Modulation of intramitochondrial free Ca2+ concentration by antagonists of Na+-Ca2+ exchange. TiPS 14 408 PMID: 8296399
White and Reynolds (1997) Mitochondria accumulate Ca2+ following intense glutamate stimulation of cultured rat forebrain neurones. J.Physiol. 498 31 PMID: 9023766
If you know of a relevant reference for CGP 37157, please let us know.
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Keywords: CGP 37157, CGP 37157 supplier, Antagonists, mitochondrial, Na+/Ca2+, Exchanger, Ca2+, Signaling, Signalling, Calcium, Sodium, Ion, Transporters, Pumps, CGP37157, NCX, 1114, Tocris Bioscience
13 Citations for CGP 37157
Citations are publications that use Tocris products. Selected citations for CGP 37157 include:
Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Elife 16 5555 PMID: 25768340
Yang et al (2015) Mitochondrial Ca2+ and membrane potential, an alternative pathway for Interleukin 6 to regulate CD4 cell effector function. J Biol Chem 4 PMID: 25974216
Pecze et al (2015) Routes of Ca2+ Shuttling during Ca2+ Oscillations: FOCUS ON THE ROLE OF MITOCHONDRIAL Ca2+ HANDLING AND CYTOSOLIC Ca2+ BUFFERS. World J Gastroenterol 290 28214 PMID: 26396196
Nikolaeva et al (2005) Na+-dependent sources of intra-axonal Ca2+ release in rat optic nerve during in vitro chemical ischemia. J Neurosci 25 9960 PMID: 16251444
Pandit et al (2012) Na delivery and ENaC mediate flow regulation of collecting duct endothelin-1 production. Am J Physiol Renal Physiol 302 F1325 PMID: 22357920
Kim et al (2006) Involvement of mitochondrial Na+-Ca2+ exchange in intestinal pacemaking activity. J Biol Chem 12 796 PMID: 16521198
Lee et al (2007) Target cell-specific involvement of presynaptic mitochondria in post-tetanic potentiation at hippocampal mossy fiber synapses. J Neurosci 27 13603 PMID: 18077672
Zhdanov et al (2011) Bafilomycin A1 activates respiration of neuronal cells via uncoupling associated with flickering depolarization of mitochondria. Cell Mol Life Sci 68 903 PMID: 20820851
Midkiff et al (2011) Small molecule inhibitors of the Candida albicans budded-to-hyphal transition act through multiple signaling pathways. PLoS One 6 e25395 PMID: 21966518
Schild et al (2003) Brain mitochondria are primed by moderate Ca2+ rise upon hypoxia/reoxygenation for functional breakdown and morphological disintegration. Am J Physiol Heart Circ Physiol 278 25454 PMID: 12702720
Bastioli et al (2019) Selective inhibition of mitochondrial sodium-calcium exchanger protects striatal neurons from α-synuclein plus rotenone induced toxicity. Cell Death Dis 10 80 PMID: 30692508
Blomeyer et al (2013) Dynamic buffering of mitochondrial Ca2+ during Ca2+ uptake and Na+-induced Ca2+ release. J Bioenerg Biomembr 45 189 PMID: 23225099
Panja et al (2019) Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity. Neuropathol Appl Neurobiol 45 141 PMID: 29679372
Do you know of a great paper that uses CGP 37157 from Tocris? Please let us know.
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