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.
All Tocris products are intended for laboratory research use only.
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 products' biological activity.
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 PMID:
Keywords: CI 988, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, CI988, PD134308, PD, 134308, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience
