ROR Antagonist

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a K_i of 220 nM.

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a K_i of 105 nM and an IC₅₀ of ~320 nM.

Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.

TMP778 is a potent and selevtive RORγt inverse agonist, with an IC₅₀ of 7 nM in FRET assay.

PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC₅₀ of 4.1 nM. Anti-skin inflammatory activity.

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.

AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.

TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC₅₀ of 0.03 μM.

Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1.

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

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

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC₅₀ of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.

RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC₅₀s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC₅₀=1.9 nM, reporter gene IC₅₀=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ).

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

RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (K_D=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells.

TMP780 is an inverse agonist of RORγt with an IC₅₀ of 13 nM. RORγt is a tractable agent target for the treatment of cutaneous inflammatory disorders.

RORγ inverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC₅₀ values of 0.4 and 0.9 μM for Gal4-RORγ and full-length RORγ, respectively. RORγ inverse agonist 2 is useful in the study of autoimmune diseases.