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Description: Potent and selective CRF1 antagonist; anxiolytic
Chemical Name: 8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
Purity: ≥98% (HPLC)
Biological Activity for Pexacerfont
Pexacerfont is a 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.
Technical Data for Pexacerfont
| M. Wt | 340.43 |
| Formula | C18H24N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 459856-18-9 |
| PubChem ID | 9884366 |
| InChI Key | LBWQSAZEYIZZCE-SNVBAGLBSA-N |
| Smiles | CC[C@H](NC1=NC(C)=NC2=C(C3=C(N=C(C=C3)OC)C)C(C)=NN12)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.
Solubility Data for Pexacerfont
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.04 | 100 | |
| ethanol | 34.04 | 100 |
Preparing Stock Solutions for Pexacerfont
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 |
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Product Datasheets for Pexacerfont
References for Pexacerfont
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
Citations for Pexacerfont
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Literature in this Area
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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.