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Category: 7TM ReceptorsarrowPeptides (Hypothalamic/Pituitary Hormones)arrowCRF Receptors
Cat.No. Product Name
2779 CP 154526
Price and Availability

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CP 154526
Chemical Name: N-Butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)- 7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride

Biological Activity:

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.

Technical Data:

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M.Wt: 400.99
Formula: C23H32N4.HCl
Storage: Desiccate at +4°C
Solubility: Soluble to 50 mM in DMSO and to 50 mM in Ethanol
Purity: >98%
CAS No: [157286-86-7]

Resources:

  • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Lundkist et al (1996) A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic activity. Eur.J.Pharmacol. 309 195. Schulz et al (1996) CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc.Natl.Acad.Sci.USA 93 10477. 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.
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    Keywords: CP 154526, Peptides (Hypothalamic / Pituitary Hormones), Selective, Non-peptide CRF1 Antagonist, CP154526, Tocris Bioscience

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