CI 988

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Cat.No. 2607 - CI 988 | C35H42N4O6 | CAS No. 130332-27-3
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% (HPLC)
Datasheet
Citations
Reviews
Literature

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
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 130332-27-3
PubChem ID 108187
InChI Key FVQSSYMRZKLFDR-ZABPBAJSSA-N
Smiles C[C@](NC(OC5C3CC(CC5C6)CC6C3)=O)(C(NC[C@@H]([C@]4=CC=CC=C4)NC(CCC(O)=O)=O)=O)CC2=CNC1=CC=CC=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 61.47 100

Preparing Stock Solutions

The following data is based on the product molecular weight 614.73. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.63 mL 8.13 mL 16.27 mL
5 mM 0.33 mL 1.63 mL 3.25 mL
10 mM 0.16 mL 0.81 mL 1.63 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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References

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

Moody et al (2001) CI-988 inhibits growth of small cell lung cancer cells. J.Pharmacol.Exp.Ther. 299 1154 PMID: 11714907

Andre et al (2005) Involvement of cholecystokininergic systems in anxiety-induced hyperalgesia in male rats: behavioral and biochemical studies. J.Neurosci. 25 7896 PMID: 16135746

Hughes et al (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc.Natl.Acad.Sci.USA 87 6728


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Citations for CI 988

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