1H-Inden-1-one, 2,3-dihydro-6-methoxy-5-(4-morpholinyl)-2-[[3-(trifluoromethyl)-2-pyridinyl]methyl]-

Description

ARN-6039 (being developed by Arrien), is a Potent, Orally Available Inverse Agonist of RORgammat for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against ROR?t was demonstrated in a ROR?t-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 release from CD4+T cell assays (220 nM). The compound also possesses ideal CNS drug-like criteria, exhibited excellent pharmacokinetics (%F: 37), pharmacodynamics, and correlative PK/PD and ADME characteristics.