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 or in human hepatocytes, Dazucorilant acts as full antagonist since it is able to prevent the dexamethasone-induced increase in TAT activity and to induce non-measurable agonist activity in the absence of dexamethasone[3].

Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity[1]. Dazucorilant (5, 10 or 20 mg/kg; i.p.) reverses hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restores the hippocampal levels of synaptic markers, reestablishes basal plasma levels of glucocorticoids and improves cognitive function at a dose of 10 mg/kg[2]. Animal Model: Wobbler mice (five-month-old)[1]Dosage: 30 mg/kg/day Administration: S.c. Result: Wobbler mice showed reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity. Animal Model: Adult SD male rats[2]Dosage: 5, 10 or 20 mg/kg Administration: I.p. Result: Reversed hippocampal amyloid-β peptide generation, neuroinflammation and apoptotic processes, restored the hippocampal levels of synaptic markers, reestablished basal plasma levels of glucocorticoids and improved cognitive function at a dose of 10 mg/kg.