RORγ Agonist

Zymostenol (5a-Cholest-8-en-3b-ol) is a late-stage precursor in the biosynthesis of cholesterol. Zymostenol is a RORγ agonist (EC₅₀: 1 μM).

RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC₅₀ of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation.

Hexyl 4-hydroxybenzoate (Hexylparaben) is a retinoic acid-related orphan receptor RORγ(t) agonist with an EC₅₀ of 144 nM. Hexyl 4-hydroxybenzoate is used in the study of autoimmune diseases.

RORγt inverse agonist 35 (Compound 22) is a RORγt inverse agonist with an IC₅₀ of 1.51 μM. RORγt inverse agonist 35 significantly inhibits Th17 differentiation and proinflammatory properties in human CD4⁺ T cells. RORγt inverse agonist 35 can be used for research of Th17-driven autoimmune diseases, such as psoriasis, multiple sclerosis, and inflammatory bowel disease (IBD).

XY039 (compound 13e) is a RORγ inverse agonist with the IC₅₀ of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro.

RORγ agonist 2 (Compound 34) is a selective RORγ agonist with an EC₅₀ of 0.03  μM for hRORγ. RORγ agonist 2 significantly inhibits tumors growth in syngeneic MC38 tumor mice model.

CD12681 (compound 14) is a potent and selective RORγ inverse agonist with IC₅₀ of 19 nM and 10 nM for RORγ GAL4 and CD4-IL-17 cells, respectively. CD12681 decreases the IL-17 inflammatory cell recruitment. CD12681 has the potential for the research of psoriasis.