Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-Indol-3-yl)-2-methyl-1-oxo-2-[[[[(1S,2R,4S)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]oxy]carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective, nonpeptide CCK2 receptor antagonist (IC50 values are 2.8 and 1232 nM for CCK2 and CCK1 respectively) that displays negligible affinity at GABAA, benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT3 receptors (IC50 > 10 μM). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats.
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
61.68
100
Preparing Stock Solutions
The following data is based on the product molecular weight 616.76. 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
1.62 mL
8.11 mL
16.21 mL
5 mM
0.32 mL
1.62 mL
3.24 mL
10 mM
0.16 mL
0.81 mL
1.62 mL
50 mM
0.03 mL
0.16 mL
0.32 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Dorre and Smith
(1998) CholecystokininB receptor antagonist increases food intake in rats. Physiol.Behav. 65 11 PMID: 9811359
Tsutsumiet al (1999) Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides 33 483 PMID: 10657528
Hugheset 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: