Discovery and Characterization of CD12681, a Potent RORγ Inverse Agonist, Preclinical Candidate for the Topical Treatment of Psoriasis
- ChemMedChem. 2018 Feb 20;13(4):321-337. doi: 10.1002/cmdc.201700758.
- 1. Nestlé Skin Health R&D, 2400 Route des Colles, BP 87, 06902, Sophia-Antipolis Cedex, France.
With possible implications in multiple autoimmune diseases, the retinoic acid receptor-related Orphan Receptor RORγ has become a sought-after target in the pharmaceutical industry. Herein are described the efforts to identify a potent RORγ inverse agonist compatible with topical application for the treatment of skin diseases. These efforts culminated in the discovery of N-(2,4-dimethylphenyl)-N-isobutyl-2-oxo-1-[(tetrahydro-2H-pyran-4-yl)methyl]-2,3-dihydro-1H-benzo[d]imidazole-5-sulfonamide (CD12681), a potent inverse agonist with in vivo activity in an IL-23-induced mouse skin inflammation model.
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Cat. No.Product NameDescriptionTargetResearch Area
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target: RORResearch Areas: Inflammation/Immunology