CD12681

CD12681 (CD-12681) is a potent, selective RORγ inverse agonist with IC50 of 19 nM, displays no activity against a panel of nuclear receptors (RORα, RARγ, LXRβ, PPARγ and VDR); inhibits IL17 production in stimulated CD4 in human hepatocytes with IC50 of 10 nM; inhibits ear swelling and IL-17 cell recruitment induced by IL-23 in mice model, CD12681 is a selective RORγ inverse agonist is sufficient to modulate an IL-23/IL-17-mediated skin inflammation.

References 1. Baffert F, et al. Mol Cancer Ther. 2010 Jul;9(7):1945-55. 2. Ringel F, et al. Acta Haematol. 2014;132(1):75-86. 3. Cheon JH, et al. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182. 4. Haissaguerre M, et al. Front Pharmacol. 2018 May 15;9:527. View Related Products by Target ROR