Top Suppliers:I want be here

1496508-34-9

1496508-34-9 structure
1496508-34-9 structure
  • Name: Dazucorilant
  • Chemical Name: Dazucorilant
  • CAS Number: 1496508-34-9
  • Molecular Formula: C29H22F4N4O3S
  • Molecular Weight: 582.57
  • Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
  • Create Date: 2022-01-09 11:33:02
  • Modify Date: 2024-01-30 13:47:32
  • Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2].

Name Dazucorilant
Description Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2].
Related Catalog
Target

GR[1]

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[3].
In Vivo 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.
References

[1]. Meyer M, et al. The Selective Glucocorticoid Receptor Modulator Cort 113176 Reduces Neurodegeneration and Neuroinflammation in Wobbler Mice Spinal Cord. Neuroscience. 2018;384:384-396.

[2]. Pineau F, et al. New selective glucocorticoid receptor modulators reverse amyloid-β peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109-122.

[3]. Canet G, et al. Central Role of Glucocorticoid Receptors in Alzheimer's Disease and Depression. Front Neurosci. 2018;12:739. Published 2018 Oct 16.

Molecular Formula C29H22F4N4O3S
Molecular Weight 582.57