1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. ROR

ROR

The retinoic acid-related orphan receptor (ROR) subgroup of nuclear receptors consists of three members, RORα, -β and -γ (NR1F1-3 or RORA-C). RORs regulate several important physiological processes and have been implicated in a number of pathologies. RORα is critical for cerebellar development and bone formation, while RORβ regulates functions in the brain and retina. RORγ plays a key role in lymph node development and thymopoiesis. Furthermore, both RORα and RORγ are involved in regulating various metabolic pathways, inflammatory responses and immune functions, including Th17 cell differentiation.

The retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ), are key regulators of helper T (Th)17 cell differentiation, which is involved in the innate immune system and autoimmune disorders. RORα/γ are members of the nuclear hormone receptor superfamily, which contains a signature type II zinc finger DNA binding motif and a hydrophobic ligand binding pocket.

ROR Isoform Specific Products:

  • RORγ

  • RORα

  • RORβ

ROR Related Products (22):

Cat. No. Product Name Effect Purity
  • HY-10626
    T0901317 Antagonist 99.91%
    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 Ki 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.
  • HY-14413
    SR3335 Antagonist 98.02%
    SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
  • HY-N0155
    Nobiletin Agonist 99.04%
    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
  • HY-104037
    Cintirorgon Agonist 99.95%
    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.
  • HY-14422
    SR1078 Agonist 99.67%
    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.
  • HY-125801
    3-Oxo-5β-cholanoic acid Inhibitor >98.0%
    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).
  • HY-103637A
    Vimirogant hydrochloride Inhibitor 98.33%
    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.
  • HY-120210
    XY018 Antagonist 99.76%
    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).
  • HY-13421
    SR1001 Inhibitor 99.84%
    SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
  • HY-120384
    AZD-0284 Antagonist 99.92%
    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.
  • HY-19770
    GSK2981278 Antagonist 99.70%
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
  • HY-12776
    GSK805 Inhibitor
    GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
  • HY-16998
    SR2211 Antagonist >98.0%
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
  • HY-101454
    SR0987 Agonist 99.56%
    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.
  • HY-112706
    PF-06747711 Antagonist 99.48%
    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.
  • 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.
  • HY-19775
    GNE-6468 Inhibitor 99.50%
    GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.
  • HY-117819
    TMP920 Antagonist 99.88%
    TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
  • 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).
  • HY-130243
    RORγt Inverse agonist 6 Antagonist
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the treatment of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
Isoform Specific Products

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