rar-related orphan receptor

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

GSK805 is a potent, orally bioavailable and CNS-penetrant RORγt inhibitor.

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active, and selective inverse agonist for RORγt with an IC50 of 63.8 nM, exhibiting improved drug-like properties[1].

Cedirogant (ABBV-157) is an orally active, retinoid-related orphan receptor-γt (RORγt) inverse agonist used in psoriasis studies.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α γ.

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor κB (NF κB).

RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.

Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).

Bevurogant is an antagonist of RORγt receptor and can be used in studies about the treatment of chronic inflammatory diseases.

1. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.

SR0987 is a RORγt agonist,

SR3335 (ML 176) is a selective inverse agonist of RORα that competitively inhibits the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).

SR 1001 is an inverse agonist for RORα RORγ (Kis: 172 111 nM).

Cintirorgon (LYC-55716) is a selective, oral agonist of RORγ, modulating gene expression in RORγ-expressing T lymphocyte immune cells.