Catalog Number: 3721
Chemical Name: 2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Biological Activity
Neurotensin antagonist; selective for NTS1 over NTS2 (apparent affinity, Ke, is 36 nM for NTS1). Competitively inhibits binding of [125I]-neurotensin to HT29 and N1E115 cell membranes (IC50 values are 15.3 and 20.4 nM respectively). Orally bioavailable.
Technical Data
  • M.Wt:
    587.07
  • Formula:
    C32H31ClN4O5
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    146362-70-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor.
    Gully et al.
    Proc.Natl.Acad.Sci.USA, 1993;90:65
  2. Characterization of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells.
    Oury-Donat et al.
    Br.J.Pharmacol., 1995;116:1899
  3. The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
    Thomas et al.
    Bioorg.Med.Chem.Lett., 2009;19:1438

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