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Submit ReviewCP 376395 hydrochloride
Description: Potent and selective CRF1 antagonist; binds at an allosteric site
Chemical Name: N-(1-Ethylpropyl)-3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-4-pyridinamine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for CP 376395 hydrochloride
CP 376395 hydrochloride is a potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively). Binds at an allosteric site. Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.
Compound Libraries for CP 376395 hydrochloride
CP 376395 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CP 376395 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CP 376395 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 18.15 | 50 | |
| DMSO | 36.29 | 100 |
Preparing Stock Solutions for CP 376395 hydrochloride
The following data is based on the product molecular weight 362.94. Batch specific molecular weights may vary from batch to batch due to the degree 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 for CP 376395 hydrochloride
References for CP 376395 hydrochloride
References are publications that support the biological activity of the product.
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
Lu et al (2019) Small molecule allosteric modulators of G-protein-coupled receptors: drug-target interactions. J.Med.Chem. 62 24 PMID: 29457894
If you know of a relevant reference for CP 376395 hydrochloride, please let us know.
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Keywords: CP 376395 hydrochloride, CP 376395 hydrochloride supplier, Potent, selective, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, CP376395, hydrochloride, negative, allosteric, modulator, NAM, 3212, Tocris Bioscience
3 Citations for CP 376395 hydrochloride
Citations are publications that use Tocris products. Selected citations for CP 376395 hydrochloride include:
Kean et al (2015) Conformational thermostabilisation of cortico. releasing factor receptor 1. Mol Pain 5 11954 PMID: 26159865
Boyson et al (2014) Social stress and CRF-DA interactions in the VTA: role in long-term escalation of cocaine self-administration. J Neurosci 34 6659 PMID: 24806691
Tran et al (2014) Importance of CRF receptor-mediated mechanisms of the bed nucleus of the stria terminalis in the processing of anxiety and pain. Neuropsychopharmacology 39 2633 PMID: 24853772
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.