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Dazucorilant

From Wikipedia, the free encyclopedia
Glucocorticoid receptor modulator
Pharmaceutical compound
Dazucorilant
Clinical data
Other namesCORT-113176
Identifiers
  • [(4aR)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanone
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC29H22F4N4O3S
Molar mass582.57 g·mol−1
3D model (JSmol)
  • 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
  • InChI=1S/C29H22F4N4O3S/c30-22-6-8-23(9-7-22)37-26-15-21-12-14-36(41(39,40)24-10-4-20(5-11-24)29(31,32)33)18-28(21,16-19(26)17-35-37)27(38)25-3-1-2-13-34-25/h1-11,13,15,17H,12,14,16,18H2/t28-/m0/s1
  • Key:VXOBXKQLNWYQPQ-NDEPHWFRSA-N

Dazucorilant (CORT-113176) is an example of aselective glucocorticoid receptor modulator that is in clinical development.[1] It is expected to have uses in the treatment ofneurodegenerative diseases,Alzheimer's disease andHuntington's chorea, for example.[2][3][4]

See also

[edit]

References

[edit]
  1. ^Hunt, H. J., Belanoff, J. K., Golding, E., Gourdet, B., Phillips, T., Swift, D., Thomas, J., Unitt, J. F., Walters, I. (December 2015). "1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile".Bioorganic & Medicinal Chemistry Letters.25 (24):5720–5725.doi:10.1016/j.bmcl.2015.10.097.PMID 26546213.
  2. ^Meyer, M., Lara, A., Hunt, H., Belanoff, J., Kloet, E. R. de, Gonzalez Deniselle, M. C., De Nicola, A. F. (August 2018). "The Selective Glucocorticoid Receptor Modulator Cort 113176 Reduces Neurodegeneration and Neuroinflammation in Wobbler Mice Spinal Cord".Neuroscience.384:384–396.doi:10.1016/j.neuroscience.2018.05.042.hdl:11336/85371.PMID 29890290.
  3. ^Meyer, M., Kruse, M. S., Garay, L., Lima, A., Roig, P., Hunt, H., Belanoff, J., Kloet, E. R. de, Deniselle, M. C. G., De Nicola, A. F. (January 2020). "Long-term effects of the glucocorticoid receptor modulator CORT113176 in murine motoneuron degeneration".Brain Research.1727 146551.doi:10.1016/j.brainres.2019.146551.PMID 31726042.
  4. ^Gentenaar, M., Meulmeester, F. L., Burg, X. R. van der, Hoekstra, A. T., Hunt, H., Kroon, J., Roon-Mom, W. M. C. van, Meijer, O. C. (April 2024). "Glucocorticoid receptor antagonist CORT113176 attenuates motor and neuropathological symptoms of Huntington's disease in R6/2 mice".Experimental Neurology.374 114675.doi:10.1016/j.expneurol.2024.114675.hdl:1887/3721107.PMID 38216109.
GRTooltip Glucocorticoid receptor
Agonists
Mixed
(SEGRMsTooltip Selective glucocorticoid receptor agonists)
Antagonists
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