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.

XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC₅₀, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).

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.

GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC₅₀ value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC₅₀ of 30 nM for IL-17 PBMC.

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC₅₀ value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

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.

(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC₅₀ of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC₅₀ of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4⁺ T cells into other lineages, including Th1 and regulatory T cells.

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.

JTE-151 is an orally active, selective RORγ antagonist with IC₅₀ values of 20.6 nM, 41.8 nM and 32.2 nM against hRORγ, rRORγ and mRORγ, respectively. JTE-151 reduces the production of IL-17. JTE-151 alleviates paw swelling and bone destruction in arthritis models. JTE-151 can be used in research related to rheumatoid arthritis, collagen-induced arthritis, experimental autoimmune encephalomyelitis, psoriasis, multiple sclerosis and inflammatory bowel disease.

SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC₅₀ value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.

GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC₅₀ of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats.

RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC₅₀ of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R

BMS-986251 is an orally active and selective RORγt inverse agonist with an EC₅₀ of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC₅₀ of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).

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.