ROR

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.

7 Items

  • XY018
    Cat. No.
    A77556

    XY018

    XY018 is a selective antagonist of ROR-γ (retinoic acid receptor-related orphan receptor gamma), designed to inhibit its constitutive activity. With an EC50 value of 190 nM in 293T cells, XY018 effectively disrupts ROR-γ signaling by binding to its hydrophobic ligand binding domain. This compound is valuable for research applications focused on autoimmune diseases, metabolic disorders, and inflammation by modulating ROR-γ activity.

    1 mg
    $30.00
    5 mg
    $65.00
    All 7 sizes
  • Bevurogant
    Cat. No.
    A77557

    Bevurogant

    Synonyms: BI 730357

    Bevurogant is a selective antagonist of the retinoid-related orphan receptor gamma t (RORγt), which plays a critical role in immune response and inflammation. This compound is primarily utilized in research focused on chronic inflammatory diseases, offering insights into therapeutic strategies for conditions such as autoimmune disorders. Its ability to modulate RORγt activity makes it a valuable tool in the study of immune regulation and potential treatment pathways.

    1 mg
    $35.00
    5 mg
    $80.00
    All 6 sizes
  • (±)-ML 209
    Cat. No.
    A77565

    (±)-ML 209

    (±)-ML 209 is a selective RORγ antagonist that effectively inhibits RORγt transcriptional activity, demonstrating an IC50 of 300 nM in HEK293t cells. This diphenylpropanamide compound specifically suppresses murine Th17 cell differentiation while leaving the differentiation of naïve CD4+ T cells into Th1 and regulatory T cell lineages unaffected. Its unique mechanism makes (±)-ML 209 a valuable tool for researchers investigating the role of RORγ in immune responses and related diseases.

    1 mg
    $75.00
    5 mg
    $180.00
    All 7 sizes
  • TMP920
    Cat. No.
    A77568

    TMP920

    TMP920 is a potent and selective antagonist of RORγt, a retinoic acid receptor-related orphan receptor involved in immune signaling. It effectively inhibits the binding of RORγt to the SRC1 peptide, demonstrating an IC50 value of 0.03 μM. TMP920 is valuable for research applications focusing on autoimmune diseases, as well as the modulation of Th17 cell differentiation and function.

    2 mg
    $25.00
    5 mg
    $65.00
    All 5 sizes
  • GNE-3500
    Cat. No.
    A77569

    GNE-3500

    GNE-3500 is a selective, orally active antagonist of Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3), exhibiting an EC50 of 12 nM. This compound demonstrates favorable pharmacokinetic properties in rat models, making it a valuable tool for research applications focused on modulating RORc-related pathways. GNE-3500 is particularly relevant for studies investigating autoimmune diseases and inflammatory responses where RORc plays a critical regulatory role.

    5 mg
    $720.00
    10 mg
    $1,175.00
    All 5 sizes
  • Retezorogant
    Cat. No.
    A77579

    Retezorogant

    Retezorogant is a selective antagonist of the retinoid-related orphan receptor gamma (RORγ). This compound plays a significant role in modulating immune responses and has potential applications in the treatment of autoimmune diseases and inflammatory conditions. Retezorogant's ability to inhibit RORγ activity makes it a valuable tool for researchers investigating the mechanisms of Th17 cell differentiation and related pathways.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • RORγ antagonist 1
    Cat. No.
    A77590

    RORγ antagonist 1

    RORγ antagonist 1 is a potent antagonist of the retinoic acid receptor-related orphan receptor gamma (RORγ) with a dissociation constant (KD) of 0.18 μM. This compound demonstrates significant anti-proliferative effects in HPAF-II pancreatic cancer xenograft models. Additionally, RORγ antagonist 1 inhibits key signaling pathways, including RAS/MAPK and AKT/mTORC1, and induces caspase-dependent apoptosis in pancreatic cancer cells, making it a valuable tool for cancer research and potential therapeutic applications.

7 Items

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