Dazucorilant (C09-1126-105)

Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor ( GR ) modulator with a K i value In VitroIn 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 VivoDazucorilant (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:SolidIC50& Target:GR. Molecular Formula: C29H22F4N4O3S Molecular Weight: 582.57 PubChem CID: 72192163 Isomeric SMILES: C1CN(C[C@@]2(C1=CC3=C(C2)C=NN3C4=CC=C(C=C4)F)C(=O)C5=CC=CC=N5)S(=O)(=O)C6=CC=C(C=C6)C(F)(F)F