2. Signaling Pathways
  3. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  4. ROR

ROR

RAR-related orphan receptor

ROR

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Retinoic acid receptor-related orphan receptors (RORs) are a subfamily of the thyroid hormone receptor, which is a subfamily of the nuclear receptors and belonging to the orphan nuclear receptor family. The ROR subfamily contains three members: RORα (NR1F1), RORβ (NR1F2), and RORγ (NR1F3) and function as ligand-dependent transcription factors.

RORs are reported to activate transcription through ligand-dependent interactions with co-regulators and are involved in the development of secondary lymphoid tissues, autoimmune diseases, inflammatory diseases, the circadian rhythm, and metabolism homeostasis.

RORα and RORγ are important regulators of the immune system. The development and differentiation of Th17 cells are dependent on these factors. RORγ is expressed in lymphoid tissue inducer cells, innate lymphoid cells, invariant natural killer T cells, and γδ T cells, which contribute to inflammation and autoimmune disease.

ROR Isoform Specific Products:

ROR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161096
    Antitumor agent-127
    		99.09%
    Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines.
    Antitumor agent-127
  • HY-138115
    7ß,27-Dihydroxycholesterol
    		Activator ≥99.0%
    7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a potent and selective activator of RORγt (Ki=120 nM). 7ß,27-Dihydroxycholesterol promotes the differentiation of mouse and human CD4+ Th17 cells. 7ß,27-Dihydroxycholesterol also increases the production of IL-17 depended on CYP27A1.
    7ß,27-Dihydroxycholesterol
  • HY-142296
    RORγt inhibitor 1
    		Inhibitor
    RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC50 value of 1 nM.
    RORγt inhibitor 1
  • HY-136527
    BMS-986251
    		Antagonist
    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).
    BMS-986251
  • HY-126321
    RORγt agonist 1
    		Agonist
    RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.
    RORγt agonist 1
  • HY-145590
    Retezorogant
    		Antagonist
    Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1.
    Retezorogant
  • HY-132900
    RORγ agonist 1
    		Agonist
    RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.
    RORγ agonist 1
  • HY-132195
    RORγt inverse agonist 14
    		Inhibitor
    RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis.
    RORγt inverse agonist 14
  • HY-128353
    ROR agonist-1
    		Antagonist
    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 TH 17 cells with a pIC50 of 7.5.
    ROR agonist-1
  • HY-152851
    Izumerogant
    		Agonist 99.95%
    Izumerogant (IMU-935) is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM.
    Izumerogant
  • HY-111748
    RORγt Inverse agonist 2
    		Antagonist
    RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM.
    RORγt Inverse agonist 2
  • HY-130243
    RORγt Inverse agonist 6
    		Antagonist 98.97%
    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.
    RORγt Inverse agonist 6
  • HY-133128
    FM26
    		Antagonist
    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.
    FM26
  • HY-128573
    RORγt Inverse agonist 3
    		Antagonist 99.93%
    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.
    RORγt Inverse agonist 3
  • HY-142806
    RORγt inverse agonist 26
    RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .
    RORγt inverse agonist 26
  • HY-111509
    TAK-828F
    		Antagonist
    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).
    TAK-828F
  • HY-126252
    A-9758
    		Inhibitor
    A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
    A-9758
  • HY-115777
    ARN-6039
    		Agonist
    ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.
    ARN-6039
  • HY-115879
    SHR168442
    		Modulator
    SHR168442 is a modulator of retinoid-related orphan receptor gamma (RORγ) with an IC50 value of 0.035 μM.
    SHR168442
  • HY-122737
    RORγt Inverse agonist 8
    		Antagonist
    RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD.
    RORγt Inverse agonist 8
Cat. No. Product Name / Synonyms Application Reactivity
ROR Isoform Comparison

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