CI 988

Catalog # Availability Size / Price Qty
2607/10
2607/50
CI 988 | CAS No. 130332-27-3 | CCK2 Receptor Antagonists
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Description: Potent and selective CCK2 antagonist
Alternative 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

Purity: ≥99%

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Biological Activity

CI 988 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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