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Category:
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7TM Receptors Peptides (Gastrointestinal)CCK Receptors
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Cat.No.
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Product Name
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2607 |
CI 988
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| Alternative name(s): |
PD 134308 |
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Price and Availability
Click here for full price details of
CI 988
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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 |
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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 mM). Exhibits anxiolytic activity
following oral administration.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
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. Moody et al (2001) CI-988 inhibits growth of small cell
lung cancer cells. J.Pharmacol.Exp.Ther. 299 1154. Andre et
al (2005) Involvement of cholecystokininergic systems in anxiety-induced
hyperalgesia in male rats: behavioral and biochemical studies. J.Neurosci. 25
7896.
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or by Research Area
Keywords: CI 988, Peptides (Gastrointestinal), Potent & Selective CCK2 Antagonist, PD 134308, CI988, Tocris Bioscience
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| “I am grateful for your honesty and courtesy. The principles of Tocris are very different to that of your competitors who, in fact, have put our inhibitor on the market without any approval, exhibiting a pirate policy and a total absence of ethics..” Researcher, University of Pisa, Italy |
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