Dazucorilant (CORT113176) is a non-steroidal glucocorticoid receptor (GR) modulator characterized by its high affinity and selectivity. With an impressive K i value of ＜1 nM in vitro, Dazucorilant proves to be an exceptional compound for investigating neurological disorders.

In HepG2 human cells and human hepatocytes, Dazucorilant functions as a full antagonist. It effectively inhibits the elevation of TAT activity triggered by dexamethasone and exhibits negligible agonist activity when dexamethasone is absent[3].

Dazucorilant, administered subcutaneously (s.c.) at a dosage of 30 mg/kg/day to five-month-old Wobbler mice, effectively reversed motoneuron abnormalities and reduced both proinflammatory mediators and glial reactivity[1]. In a separate study, intraperitoneal (i.p.) administration of Dazucorilant at doses of 5, 10, or 20 mg/kg in adult SD male rats led to a reversal of hippocampal amyloid-β peptide accumulation, neuroinflammation, and apoptotic processes. Additionally, it restored synaptic marker levels in the hippocampus, normalized basal plasma glucocorticoid levels, and enhanced cognitive function, with the optimal results observed at the 10 mg/kg dosage[2].