Biological Activity
Potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively). Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.
Compound Libraries
CP 376395 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 362.94 |
| Formula | C21H30N2O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1013933-37-3 |
| PubChem ID | 24806455 |
| InChI Key | UDIOZDHQQNYISB-UHFFFAOYSA-N |
| Smiles | CC1=CC(NC(CC)CC)=C(C)C(OC2=C(C)C=C(C)C=C2C)=N1.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 | |||
| 1eq. HCl | 36.29 | 100 | |
| DMSO | 36.29 | 100 | |
| ethanol | 36.29 | 100 | |
| water | 18.15 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 362.94. 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 | 2.76 mL | 13.78 mL | 27.55 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.51 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chen et al (2008) 2-Aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J.Med.Chem. 51 1385 PMID: 18288792
Hollenstein et al (2013) Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature 499 438 PMID: 23863939
Keywords: CP 376395 hydrochloride, supplier, Potent, selective, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, CP376395, hydrochloride, CRF1, Receptors, CRF1, Receptors, Tocris Bioscience
