Catalog Number: 2779
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
  • M.Wt:
    400.99
  • Formula:
    C23H32N4.HCl
  • Solubility:
    Soluble to 50 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    257639-98-8
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic activity.
    Lundkist et al.
    Eur.J.Pharmacol., 1996;309:195
  2. Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression.
    Hodgson et al.
    Pharmacol.Biochem.Behav., 2007;86:431
  3. CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.
    Schulz et al.
    Proc.Natl.Acad.Sci.USA, 1996;93:10477
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CP 154526 include:

1 Citations: Showing 1 - 1

  1. CRF-R1 activation in the anterior-dorsal BNST induces maternal neglect in lactating rats via an HPA axis-independent central mechanism.
    Authors: Klampfl Et al.
    Biochem Biophys Res Commun 2016;64:89

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