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

ROR

RAR-related orphan receptor

ROR

Related Products

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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-102075A
    TMP778
    		Antagonist 99.99%
    TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
    TMP778
  • HY-113345
    Zymostenol
    		Agonist ≥99.0%
    Zymostenol (5a-Cholest-8-en-3b-ol) is a late-stage precursor in the biosynthesis of cholesterol. Zymostenol is a RORγ agonist (EC50: 1 μM).
    Zymostenol
  • HY-103637A
    Vimirogant hydrochloride
    		Inhibitor 98.39%
    Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
    Vimirogant hydrochloride
  • HY-128604
    XY101
    		Inhibitor 98.88%
    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
    XY101
  • HY-119366
    S18-000003
    		Inhibitor 99.31%
    S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations.
    S18-000003
  • HY-119464
    MRL-871
    		Agonist 98.18%
    MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 12.7 nM. MRL-871 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
    MRL-871
  • HY-142938
    RORγt agonist 3
    		Agonist 98.12%
    RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23).
    RORγt agonist 3
  • 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-132810
    Bevurogant
    		Antagonist 98.57%
    Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.
    Bevurogant
  • HY-133552
    RORγt Inverse agonist 10
    		Antagonist 99.13%
    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
    RORγt Inverse agonist 10
  • HY-139847
    RORγt inverse agonist 23
    		Agonist 99.34%
    RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
    RORγt inverse agonist 23
  • HY-120785
    SR1555
    		Antagonist
    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.
    SR1555
  • 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
    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
ROR Isoform Comparison

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