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

ROR

RAR-related orphan receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-163436
    F44-A13
    Antagonist
    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.
    F44-A13
  • HY-120384
    AZD-0284
    Antagonist 99.90%
    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.
    AZD-0284
  • HY-112706
    PF-06747711
    Antagonist 99.83%
    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.
    PF-06747711
  • HY-132810
    Bevurogant
    Antagonist 99.54%
    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-19770
    GSK2981278
    Antagonist 99.51%
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
    GSK2981278
  • HY-119464
    MRL-871
    Agonist 99.11%
    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-152851
    Izumerogant
    Inhibitor 99.95%
    Izumerogant (IMU-935) is an orally active RORγ/DHODH dual inhibitor with IC50s of 10 and 98 nM against RORγ and DHODH. Izumerogant efficiently blocks the replication of SARS-CoV-2, HCMV and HAdV5 with EC50 values between 3.6 and 17 nM. Izumerogant can be used for researching antiviral properties.
    Izumerogant
  • HY-49076
    RORγ inverse agonist 1
    Modulator 99.46%
    RORγ inverse agonist 1 is the inverse agonist of RORγ.
    RORγ inverse agonist 1
  • HY-137434
    Cedirogant
    Inhibitor 98.66%
    Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.
    Cedirogant
  • HY-131338
    RORγt inverse agonist 13
    Inhibitor 98.13%
    RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC50 of 63.8 nM.
    RORγt inverse agonist 13
  • HY-120785
    SR1555
    Antagonist 99.69%
    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-126037
    (±)-ML 209
    Antagonist 99.87%
    (±)-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.
    (±)-ML 209
  • HY-16983
    GNE-3500
    Antagonist 98.90%
    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.
    GNE-3500
  • 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-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-19774
    GNE-0946
    Inhibitor 98.09%
    GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
    GNE-0946
  • HY-P991209
    Nebratamig
    Inhibitor
    Nebratamig (GNC-035) is an anti-ROR1/anti-CD3/anti-PD-L1/anti-4-1BB tetra-specific antibody with potential immunostimulatory and antineoplastic activities.
    Nebratamig
  • HY-128604
    XY101
    Inhibitor 99.65%
    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-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-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
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