Cayman Pexacerfont

Pexacerfont is an antagonist of corticotropin-releasing factor receptor 1 (CRF₁; IC₅₀ = 6.1 nM for the human receptor).¹ It is selective for CRF₁ in IMR-32 cells (mean IC₅₀ = 10.6 nM) over CFR_2β 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.

WARNING This product is not for human or veterinary use.