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Potent and selective corticotropin-releasing factor 1 receptor (CRF1) antagonist (IC50 = 6.1 nM). Displays >150 fold selectivity for CRF1 over CRF2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC50 = 129 nM). Displays anxiolytic effects in rat behavioral paradigms.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 340.43. 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||2.94 mL||14.69 mL||29.37 mL|
|5 mM||0.59 mL||2.94 mL||5.87 mL|
|10 mM||0.29 mL||1.47 mL||2.94 mL|
|50 mM||0.06 mL||0.29 mL||0.59 mL|
References are publications that support the biological activity of the product.
Gilligan et al (2009) Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. J.Med.Chem. 52 3084 PMID: 19361209
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Keywords: Pexacerfont, Pexacerfont supplier, BMS, 562086, BMS562086, corticotrophin, releasing, hormone, receptor, 1, antagonists, antagonism, CRF1, anxiolytic, Receptors, 6451, Tocris Bioscience
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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* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Peptide Hormone Receptors Product ListingUpdated
A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:
- Anterior Pituitary Regulation
- Blood Pressure Regulation
- Feeding and Appetite Regulation
- Glucose Regulation
- Peptide Hormone Processing
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.