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Selective, non-peptide CRF1 receptor antagonist (Ki values are 2.7 and > 10000 nM for CRF1 and CRF2 receptors respectively). Blocks CRF-induced adenylate cyclase activation (Ki = 3.7 nM) and attenuates activation of the HPA axis by CRF. Displays anxiolytic-like activity in the rat elevated plus-maze test; brain penetrant.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 400.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.99 mL||24.94 mL||49.88 mL|
|2.5 mM||1 mL||4.99 mL||9.98 mL|
|5 mM||0.5 mL||2.49 mL||4.99 mL|
|25 mM||0.1 mL||0.5 mL||1 mL|
References are publications that support the biological activity of the product.
Lundkist et al (1996) A non peptidic cortico. releasing factor receptor antagonist attenuates fever and exhibits anxiolytic activity. Eur.J.Pharmacol. 309 195 PMID: 8874139
Hodgson et al (2007) Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression. Pharmacol.Biochem.Behav. 86 431 PMID: 17291571
Schulz et al (1996) CP-154,526: a potent and selective nonpeptide antagonist of cortico. releasing factor receptors. Proc.Natl.Acad.Sci.USA 93 10477
If you know of a relevant reference for CP 154526, please let us know.
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Keywords: CP 154526, CP 154526 supplier, Selective, non-peptide, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, CP154526, Pfizer, 2779, Tocris Bioscience
1 Citation for CP 154526
Citations are publications that use Tocris products. Selected citations for CP 154526 include:
Klampfl et al (2016) CRF-R1 activation in the anterior-dorsal BNST induces maternal neglect in lactating rats via an HPA axis-independent central mechanism. Biochem Biophys Res Commun 64 89 PMID: 26630389
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.