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

ROR

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 Related Products (69):

Cat. No. Product Name Effect Purity
  • HY-14422
    SR1078 Agonist 99.46%
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription[1][2].
  • HY-10626
    T0901317 Antagonist 99.89%
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα[1]. T0901317 activates FXR with an EC50 of 5 μM[2]. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice[4][5].
  • HY-12776
    GSK805 Inhibitor 98.26%
    GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity[1].
  • HY-104037
    Cintirorgon Agonist 98.53%
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival[1][2].
  • HY-14413
    SR3335 Antagonist 98.06%
    SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM[1][2].
  • HY-113345
    Zymostenol Agonist
    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)[1][2][3].
  • HY-139780
    JNJ-61803534 Inhibitor 99.88%
    JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6  nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions[1].
  • HY-138115
    7ß,27-Dihydroxycholesterol Activator
    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[1].
  • 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.
  • 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)[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[1][2].
  • HY-125801
    3-Oxo-5β-cholanoic acid Inhibitor
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM)[1].
  • HY-101454
    SR0987 Agonist 99.54%
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1[1].
  • HY-119464
    MRL-871 Agonist
    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[1].
  • HY-142940
    RORγt modulator 5 Modulator
    RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2)[1].
  • HY-117819
    TMP920 Antagonist 99.81%
    TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM[1].
  • 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[1].
  • HY-102075B
    TMP780 Antagonist 99.51%
    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[1].
  • HY-102075A
    TMP778 Antagonist 99.41%
    TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
  • 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[1].