Dazucorilant

Dazucorilant

Clinical data
Other names	CORT-113176
Identifiers
IUPAC name [(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	1496508-34-9
PubChem CID	72192163
DrugBank	DB18025
UNII	HR4RD5RBJ6
KEGG	D12638
ChEMBL	ChEMBL3734774
Chemical and physical data
Formula	C29H22F4N4O3S
Molar mass	582.57 g·mol−1
3D model (JSmol)	Interactive image
SMILES 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 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 (Cort113176) 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

• Nivazol – has the same pyrazole ring moiety.

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.