Formulation: A crystalline solid
Formal 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%
Formula Markup: C18H24N6O
Formula Weight: 340,4
Shelf life (days): 1460
CAS Number: 459856-18-9
Notes: Pexacerfont is an antagonist of corticotropin-releasing factor receptor 1 (CRF1; IC50 = 6.1 nM for the human receptor).{54747} It is selective for CRF1 in IMR-32 cells (mean IC50 = 10.6 nM) over CFR2β receptors endogenously expressed in pig choroid plexus membranes (IC50 = >1,000 nM) in radioligand binding assays and does not bind to the human CRF binding protein (IC50 = >1,000 nM). Pexacerfont inhibits adrenocorticotropic hormone (ACTH) release induced by CRF in primary rat pituitary cells with an IC50 value of 129 nM. It increases the time spent in the open arms of the elevated plus maze (EPM) in rats, indicating anxiolytic-like activity, when administered at doses ranging from 10 to 30 mg/kg.
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