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Description: GNE-6468 is a novel, potent and selective RORgamma (RORc) agonists with an EC50 value of 13 nM in HEK-293 cells. he nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORgamma, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine interleukin-17. GNE-0946 displayed > 300-fold selectivity for RORc over the other ROR family members, PPARgamma, and NRs in our cellular selectivity panel. The favorable potency, selectivity, and physiochemical properties of GNE-0946 and GNE-6468, in addition to their potent suppression of IL-17 production in human primary cells, support their use as chemical biology tools to further explore the role of RORc in human biology.
References: Bioorg Med Chem Lett. 2015 Aug 1; 25(15):2907-12.
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