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ROR modulators target retinoic acid receptor-related orphan receptors (RORs), a family of nuclear receptors. The family has three members, RORα, RORβ and RORγ, which bind ROR response elements in target genes and are active without an added ligand. RORα contributes to circadian clock regulation, and the immune isoform RORγt directs the differentiation of interleukin-17 (IL-17)-producing T helper (Th17) cells. In 2011 the synthetic RORα/γ ligand SR1001 was shown to suppress Th17 differentiation and autoimmunity in mice. SR-2211 and XY101 act on RORγ, whereas SR3335 is selective for RORα. SR1078 is used as an agonist of RORα and RORγ in studies of target gene expression. Related receptors without well-defined ligands are listed under Orphan Nuclear Receptor.
RORγ modulator 1 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124.
Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
SHR168442 is a selective modulator of retinoid-related orphan receptor gamma (RORγ), exhibiting an IC50 value of 0.035 μM. This compound significantly influences RORγ activity, making it valuable for research applications related to immune response and inflammatory diseases. Its precise modulation of RORγ provides insights into pathways regulated by this receptor, facilitating studies in cellular signaling and potential therapeutic interventions.
RORγt modulator 5 is a selective modulator of the RORγt nuclear receptor, exhibiting a Ki value of less than 100 nM. This compound has demonstrated potential in the study of inflammatory, metabolic, and autoimmune diseases that are mediated by RORγt. Its ability to influence RORγt signaling pathways makes it a valuable tool for researchers investigating these disease mechanisms.
RORγt modulator 2 is a selective modulator of retinoid-related orphan receptor γt (RORγt), exhibiting an IC50 of less than 50 nM. This compound is valuable for investigating RORγt-mediated pathologies including pain, inflammation, chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative disorders, and cancer. Research on RORγt modulator 2 can contribute to understanding therapeutic approaches targeting these conditions.
RORγt modulator 4 is an effective modulator of the RORγt pathway. It has been shown to influence IL-17A production in cells derived from mouse spleen, thereby contributing to research in autoimmune diseases and inflammation. This compound is valuable for studies aimed at understanding the role of RORγt in T cell differentiation and related biological processes.
RORγt Modulator 3 is a selective modulator of the retinoic acid receptor-related orphan receptor gamma t (RORγt). This compound exhibits significant biological activity in the modulation of immune responses, making it valuable for research into RORγt-mediated diseases, including pain, inflammation, chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative disorders, and various cancer types. Its application may facilitate the development of novel therapeutic strategies targeting RORγt pathways.
RORC modulator-1 is a selective modulator of the retinoic acid receptor-related orphan receptor C (RORC). It demonstrates the ability to regulate RORC activity, impacting the expression of genes involved in immune response and inflammation. This compound is valuable for research applications focused on T helper cell differentiation, autoimmune diseases, and the study of related signaling pathways.
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