ror

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

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].

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

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].

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).

ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), demonstrating inhibition of IL-17A production from human primary TH17 cells with a pIC50 of 7.5.

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.

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.

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.

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).

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).

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

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

ROR Modulator I is the first potent inverse agonist of the retinoid-related orphan receptor. It also has dual selectivity for RORβ and RORγt.

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

RORγt agonist 1 is a potent, orally bioavailable agonist of RORγt(EC50 of 20.8 nM).

RORγt Inverse Agonist 3 is a potent, selective, and orally active inverse agonist of RORγ with EC50 values of 0.22 μM for hRORγ and 0.15 μM for RORγt (human IL-17 cells), respectively.

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist (human RORγt-LBD) with an IC50 of 19 nM.

RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt, with an EC50 of 119 nM.