ChemicalBook Product Catalog API Hormones and the Endocrine System Adrenal corticosteroids Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl-

Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl-

Product NameMethanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl-
CAS1496508-34-9
MFC29H22F4N4O3S
MW582.57
EINECS
MOL File1496508-34-9.mol

Chemical Properties

Boiling point	692.9±65.0 °C(Predicted)
Density	1.46±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
form	Solid
pka	3.35±0.10(Predicted)
color	Off-white to light yellow

Usage And Synthesis

Uses

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].

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. DOI:10.1016/j.neuroscience.2018.05.042
[2] Pineau F, et al. New selective glucocorticoid receptor modulators reverse amyloid-β peptide-induced hippocampus toxicity. Neurobiol Aging. 2016;45:109-122. DOI:10.1016/j.neurobiolaging.2016.05.018
[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. DOI:10.3389/fnins.2018.00739

Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl- Supplier

Related Product Information

Send Inquriy