Glucocorticoid Receptors

Glucocorticoid receptor agonists and antagonists act on the nuclear receptor activated by cortisol. The glucocorticoid receptor (GR) is a ligand-activated transcription factor that controls genes for metabolism, stress responses and inflammation. Cloning of the human GR complementary DNA in 1985 placed it in the steroid hormone receptor family. A 2002 crystal structure of its ligand-binding domain with dexamethasone revealed a new dimer interface and mode of coactivator binding. The category covers the endogenous hormone hydrocortisone (cortisol) and synthetic agonists such as dexamethasone, budesonide and fluticasone propionate. The antagonist mifepristone, by contrast, blocks both glucocorticoid and progesterone receptors. Some entries act mainly on other targets, such as the progestin levonorgestrel and GANT61, an antagonist of glioma-associated oncogene (GLI) transcription factors.

5 Items

  • PF-04308515
    Cat. No.
    A36026

    PF-04308515

    Synonyms: PF 4308515

    PF-04308515 is a selective glucocorticoid receptor ligand that exhibits significant anti-inflammatory properties. It effectively inhibits the production of interleukin-6 (IL-6) and interferon gamma (IFNγ), making it a valuable tool for studying inflammation and immune responses. Additionally, PF-04308515 induces a weak interaction with PGC1α, providing insights into its potential metabolic effects. This compound is useful for research applications focused on inflammation, autoimmune diseases, and glucocorticoid signaling pathways.

    Out of stock

    All 3 sizes
  • Glucocorticoid receptor agonist-2 Ala-Ala-Mal
    Cat. No.
    A41373

    Glucocorticoid receptor agonist-2 Ala-Ala-Mal

    Glucocorticoid receptor agonist-2 Ala-Ala-Mal acts as an active reference for ABBV-3373 and serves as a ligand for the glucocorticoid receptor. This compound is instrumental in the synthesis of antibody-drug conjugates (ADCs) with anti-inflammatory properties. Its ability to modulate glucocorticoid receptor activity makes it a valuable reagent in the development of therapeutics targeting inflammatory diseases.

    1 mg
    $225.00
    5 mg
    $640.00
    All 3 sizes
  • Methylprednisolone aceponate
    Cat. No.
    A64706

    Methylprednisolone aceponate

    Synonyms: ZK 91588; MPA

    Methylprednisolone aceponate is a glucocorticoid with a specific mechanism of action as a selective glucocorticoid receptor ligand, primarily functioning as an anti-inflammatory agent. It exhibits weak systemic effects, making it particularly useful in the treatment of localized inflammatory conditions. This compound is valuable for research applications targeting eczema and other inflammatory skin disorders, aiding in the understanding of their pathophysiology and potential treatments.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • (Rac)-GSK866
    Cat. No.
    A64812

    (Rac)-GSK866

    Synonyms: GSK47866A

    (Rac)-GSK866 is a non-steroidal ligand that targets the glucocorticoid receptor (GR). This compound serves as an important tool for investigating GR functionality by providing insights into ligand binding mechanisms. The crystal structure of (Rac)-GSK866 in complex with the GR ligand-binding domain (PDB: 3E7C) can facilitate the exploration of GR-targeted therapeutic strategies and the development of novel GR modulators.

    25 mg
    $2,160.00
    50 mg
    $2,770.00
    All 3 sizes
  • Win 45164
    Cat. No.
    A64822

    Win 45164

    Win 45164 is an orally active ligand of the glucocorticoid receptor, primarily known for its inhibitory effects on the pituitary-adrenal axis. It promotes liver glycogen deposition and thymus involution in adrenalectomized male rats, highlighting its physiological relevance. Additionally, Win 45164 exhibits significant anti-inflammatory properties, making it a valuable tool for research in inflammatory and neurological diseases.

    Out of stock

    All 3 sizes

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