Product overview

Name CGP 37157
Description Potent, selective mitochondria Na+ / Ca2+ exchange inhibitor
Biological description 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.
Purity >99%
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Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name 7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
Molecular Weight 324.22
Chemical structure Product image
Molecular Formula C15H11Cl2NOS
CAS Number 75450-34-9
PubChem identifier 2688
SMILES C1C(=O)NC2=C(C=C(C=C2)Cl)C(S1)C3=CC=CC=C3Cl
InChi 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)
InChiKey KQEPIRKXSUIUTH-UHFFFAOYSA-N
MDL number MFCD09055422

References for CGP 37157

References are publications that support the biological activity of the product
  • 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.
  • 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.
  • 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.
  • 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.