ROR Agonist

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.

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.

RS-2982 is a retinoic acid receptor-related orphan receptor A (RORA) agonist. RS-2982 enhances the promoter activity of MIR122 via the RORA binding site, and promotes the expression and secretion of MIR122. RS-2982 reduces the expression of hepatic triglyceride biosynthetic enzymes, hepatic lipotoxicity, hepatic fibrosis and body weight in diet-fed mice, while improving insulin resistance. RS-2982 can be used in the research of non-alcoholic steatohepatitis.

AZ-5104 GMP is a GMP-grade form of AZ-5104 (HY-B0793). AZ-5104 is an orally active RORγ receptor-active compound, and also a circulating metabolite of AZD9291. AZ-5104 inhibits sensitizing EGFR mutants, EGFR^T790M drug-resistant EGFR mutants and wild-type EGFR, while showing no activity against the IGF-1R family. AZ-5104 can be used in the research of non-small cell lung cancer.

Neoruscogenin, a member of the steroidal sapogenin family, is a high-affinity agonist of the nuclear receptor RORα (NR1F1) (EC₅₀ = 0.11 µM).

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.

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.

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.

RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.

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 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.

RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC₅₀ = 21 nM) with antitumor activity.

ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.

XY077 (compound 14a) is a RORγ inverse agonist with the IC₅₀ of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro.

RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17).

RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma.

Nobiletin (Standard) is the analytical standard of Nobiletin. This product is intended for research and analytical applications. 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.

Oxyphenbutazone (monohydrate) (Standard) is the analytical standard of Oxyphenbutazone (monohydrate). This product is intended for research and analytical applications. Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis.

Cintirorgon (Standard) is the analytical standard of Cintirorgon (HY-104037). This product is intended for research and analytical applications. 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 sodium is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon sodium (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.