Catalog Number: 2607
Alternate Names: PD 134308
Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
Biological Activity
Potent and selective CCK2 (CCK-B) receptor antagonist that displays ~ 1600-fold selectivity over CCK1 receptors (IC50 values are 1.7 and 2717 nM for CCK2 and CCK1 respectively). Has negligible affinity at a range of other binding sites (IC50 > 10 μM). Exhibits anxiolytic activity following oral administration.
Technical Data
  • M.Wt:
    614.73
  • Formula:
    C35H42N4O6
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    130332-27-3
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. CI-988 inhibits growth of small cell lung cancer cells.
    Moody et al.
    J.Pharmacol.Exp.Ther., 2001;299:1154
  2. Involvement of cholecystokininergic systems in anxiety-induced hyperalgesia in male rats: behavioral and biochemical studies.
    Andre et al.
    J.Neurosci., 2005;25:7896
  3. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
    Hughes et al.
    Proc.Natl.Acad.Sci.USA, 1990;87:6728

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