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-10626
    T0901317
    Antagonist 99.85%
    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.
    T0901317
  • HY-N0155
    Nobiletin
    Agonist 99.79%
    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.
    Nobiletin
  • HY-14422
    SR1078
    Agonist 99.75%
    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.
    SR1078
  • HY-NP013
    Oxidized low density lipoprotein (mouse)
    Inducer 98.00%
    Oxidized low density lipoprotein (mouse) (Mouse ox-LDL) is an oxidized low density lipoprotein (LDL). Oxidized low density lipoprotein (mouse) induces atherosclerosis (AS) by facilitating endothelial dysfunction and accelerating the VSMCs growth and migration. Oxidized low density lipoprotein (mouse) can be used to construct an in vitro model of AS.
    Oxidized low density lipoprotein (mouse)
  • HY-125801
    3-Oxo-5β-cholanoic acid
    Inhibitor 99.37%
    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).
    3-Oxo-5β-cholanoic acid
  • HY-125801S
    3-Oxo-5β-cholanoic acid-d4
    3-Oxo-5β-cholanoic acid-d4 (Dehydrolithocholic acid-d4) is the deuterium labeled 3-Oxo-5β-cholanoic acid (HY-125801). 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).
    3-Oxo-5β-cholanoic acid-d<sub>4</sub>
  • HY-P992337
    CS5001 Antibody
    Inhibitor
    CS5001 Antibody is an IgG1 human monoclonal antibody targeting ROR1. CS5001 Antibody can be used for the synthesis of the ADC CS5001. It is applicable to research related to advanced solid tumors and lymphomas. The recommended isotype control is human IgG1 kappa (HY-P99001).
    CS5001 Antibody
  • HY-177109
    BL20-MMAE
    Inhibitor
    BL20-MMAE is an antibody-drug conjugate targeting ROR1, which is formed by conjugating an anti-ROR1 antibody with the Auristatin payload MMAE (HY-15162) via a BL20 linker.
    BL20-MMAE
  • HY-P99201
    Zilovertamab
    Inhibitor 98.21%
    Zilovertamab (UC-961) is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.
    Zilovertamab
  • HY-14413
    SR3335
    Antagonist 98.49%
    SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
    SR3335
  • HY-12776
    GSK805
    Inhibitor 99.83%
    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.
    GSK805
  • HY-113238A
    Lithocholic acid 3-sulfate disodium
    Ligand 99.93%
    Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC50 values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn2+, and 0.88 μM and 0.97 μM in the presence of Zn2+. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn2+-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases.
    Lithocholic acid 3-sulfate disodium
  • HY-143712
    Allolithocholic acid
    Inhibitor 99.69%
    Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease.
    Allolithocholic acid
  • HY-13421
    SR1001
    Inhibitor 99.84%
    SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
    SR1001
  • HY-P99828
    Cofetuzumab
    Modulator 99.31%
    Cofetuzumab (PF-06523435) is a humanized IgG1-κ monoclonal antibody targeting PTK7. The expression system of Cofetuzumab is typically CHO (Chinese hamster ovary) cells. Cofetuzumab downregulates PTK7 expression, modulates its downstream signaling pathways, and inhibits tumor sphere formation of ovarian cancer cells. Cofetuzumab can be used to synthesize the ADC molecule Cofetuzumab pelidotin (HY-P99829). Cofetuzumab is applicable to the research of tumors such as ovarian cancer.
    Cofetuzumab
  • HY-N2253
    Neoruscogenin
    Agonist 99.21%
    Neoruscogenin, a member of the steroidal sapogenin family, is a high-affinity agonist of the nuclear receptor RORα (NR1F1) (EC50 = 0.11 µM).
    Neoruscogenin
  • HY-139534
    ARI-1
    Inhibitor 99.16%
    ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. ARI-1 upregulates cleaved-PARP and p-P38. ARI-1 induces Apoptosis. ARI-1 has anticancer activity against non-small cell lung cancer.
    ARI-1
  • HY-16998
    SR2211
    Antagonist 98.90%
    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.
    SR2211
  • HY-104037
    Cintirorgon
    Agonist 99.14%
    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.
    Cintirorgon
  • HY-120210
    XY018
    Antagonist 99.68%
    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).
    XY018
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