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Images
CGP 37157 product vial image | Hello Bio
CGP 37157 product vial image | Hello Bio
Biological Data
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Biological description
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Potent and selective mitochondria Na+ / Ca2+ exchange inhibitor (IC50 = 0.36 µM). Also inhibits sarco/endoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and activates ryanodine receptor channels (RyRs) (EC50 values are 9.4 and 12.0 µM for cardiac and skeletal RyRs respectively). Displays neuroprotective properties. |
Solubility & Handling
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Storage instructions
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Room temperature |
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Solubility overview
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Soluble in DMSO (100mM) |
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Important
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This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
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Chemical name
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7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one |
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Chemical structure
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Molecular Formula
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C15H11Cl2NOS |
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SMILES
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C1C(=O)NC2=C(C=C(C=C2)Cl)C(S1)C3=CC=CC=C3Cl |
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InChi
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InChI=1S/C15H11Cl2NOS/c16-9-5-6-13-11(7-9)15(20-8-14(19)18-13)10-3-1-2-4-12(10)17/h1-7,15H,8H2,(H,18,19) |
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InChiKey
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KQEPIRKXSUIUTH-UHFFFAOYSA-N |
References for CGP 37157
References are publications that support the biological activity of the product
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CGP37157, an inhibitor of the mitochondrial Na+/Ca2+ exchanger, protects neurons from excitotoxicity by blocking voltage-gated Ca2+ channels.
Ruiz A et al (2014)
Cell Death Dis 5 : e1156.
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Benzothiazepine CGP37157 and its isosteric 2'-methyl analogue provide neuroprotection and block cell calcium entry.
González-Lafuente L et al (2012)
ACS Chem Neurosci 3(7) : 519-29.
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CGP-37157 inhibits the sarcoplasmic reticulum Ca?+ ATPase and activates ryanodine receptor channels in striated muscle.
Neumann JT et al (2011)
Mol Pharmacol 79(1) : 141-7.
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Selectivity of inhibition of Na(+)-Ca2+ exchange of heart mitochondria by benzothiazepine CGP-37157.
Cox DA et al (1993)
J Cardiovasc Pharmacol 21(4) : 595-9.
Potent, selective mitochondria Na+ / Ca2+ exchange inhibitor