CP 154526

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Cat.No. 2779 - CP 154526 | C23H32N4.HCl | CAS No. 257639-98-8
Description: Selective, non-peptide CRF1 antagonist
Chemical Name: N-Butyl-N-ethyl-2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 400.99
Formula C23H32N4.HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 257639-98-8
PubChem ID 11475094
InChI Key ZWDLBNCJWNENFF-UHFFFAOYSA-N
Smiles CC1=CN(C3=C(C)C=C(C)C=C3C)C2=C1C(N(CC)CCCC)=NC(C)=N2.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.05 50
ethanol 20.05 50

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 solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Lundkist et al (1996) A non peptidic corticotropin 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 corticotropin releasing factor receptors. Proc.Natl.Acad.Sci.USA 93 10477


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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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