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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
If you know of a relevant reference for CI 988, please let us know.
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Keywords: CI 988, CI 988 supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, CI988, PD134308, PD, 134308, Receptor, 2607, Tocris Bioscience
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.