ror-β

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

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].

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

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).

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

A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.

FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. FM26 is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM.

Methyl-3β-hydroxycholenate (Methyl 3beta-hydroxychol-5-enoate) is a modulator of RORγ.

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.

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

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.

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 1.9 nM and a reporter gene IC50 of 6.1 nM.

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

TMP778 is an effective and selective RORγt inverse agonist (IC50: 7 nM in FRET assay).

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.

GNE-0946 is a potent and selective agonist of RORγ, with an EC50 of 4 nM in HEK-293 cells.

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

PF-06747711 is an effective and selective retinoic acid receptor-related orphan C2 inverse agonist (IC50: 4.1 nM). PF-06747711 also has anti-skin inflammatory activity.