Dazucorilant

Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor ( GR ) modulator with a K i value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Dazucorilant (30 mg/kg/day; s.c.) makes mice show reversed abnormalities of motoneurons and down-regulated proinflammatory mediators and glial reactivity . 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Wobbler mice (five-month-old) 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 ratsDosage: 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. Form:Solid IC50& Target:GR

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