Dazucorilant

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
PubChem CID
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 a selective glucocorticoid receptor modulator that is in clinical development.[1] It is expected to have uses in the treatment of neurodegenerative diseases, Alzheimer's disease and Huntington's chorea, for example.[2][3][4]

See also

References

  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.
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