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.
All Tocris products are intended for laboratory research use only.
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 |
|---|---|---|---|
| 1 mM | 2.49 mL | 12.47 mL | 24.94 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.99 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 PMID:
Keywords: CP 154526, supplier, Selective, non-peptide, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, CP154526, Pfizer, CRF1, Receptors, CRF1, Receptors, Tocris Bioscience
