CGP 37157

(HB1132)

Product overview

  • Name
    CGP 37157
  • Short 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.
  • Biological action
    Inhibitor
  • Purity
    >99%
  • Our products in action

Properties

  • Chemical name
    7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one
  • Molecular Weight
    324.22
  • Chemical structure
    CGP 37157  [75450-34-9]
  • 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

Storing and Using Your Product

  • 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.

References for CGP 37157

  • 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.
    PubMedID: 22860221
  • 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.
    PubMedID: 24722281
  • 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.
    PubMedID: 7681905
  • 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.
    PubMedID: 20923851

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