1. Signaling Pathways
  2. GPCR/G Protein
  3. Glucocorticoid Receptor

Glucocorticoid Receptor

Glucocorticoid Receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response. When the glucocorticoid receptor binds to glucocorticoids, its primary mechanism of action is the regulation of gene transcription. The unbound receptor resides in the cytosol of the cell. After the receptor is bound to glucocorticoid, the receptor-glucorticoid complex can take either of two paths. The activated GR complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus. Dexamethasone is an agonist, and RU486 and cyproterone acetate are antagonists of the GR. Also, progesterone and DHEA have antagonist effects on the GR.

Glucocorticoid Receptor Related Products (68):

Cat. No. Product Name Effect Purity
  • HY-14648
    Dexamethasone Agonist 99.86%
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18L expression on monocytes.
  • HY-N0583
    Hydrocortisone Agonist 99.90%
    Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
  • HY-13683
    Mifepristone Antagonist 98.67%
    Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
  • HY-B1618
    Corticosterone Agonist 99.70%
    Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
  • HY-B0469
    Medroxyprogesterone acetate 99.82%
    Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors
  • HY-109017
    Vamorolone Agonist
    Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects.
  • HY-12946
    BI 653048 Inhibitor
    BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
  • HY-B0727
    Betamethasone valerate Agonist
    Betamethasone valerate (Betamethasone 17-valerate), the 17-valerate ester of Betamethasone, is a topical corticosteroid with anti-inflammatory activity. Betamethasone valerate is used in the treatment of recurrent aphthous stomatitis. Betamethasone valerate inhibits the binding of the radiolabeled glucocorticoid dexamethasone (3H dexamethasone) to human epidermis and mouse skin with IC50s of 5 and 6 nM, respectively.
  • HY-B1829A
    Dexamethasone phosphate disodium Agonist 99.68%
    Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.
  • HY-B0260
    Methylprednisolone Agonist 99.67%
    Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.
  • HY-17463
    Prednisolone Agonist 99.92%
    Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
  • HY-B0214
    Prednisone Agonist 99.35%
    Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
  • HY-17461
    Cortisone Agonist 99.90%
    Cortisone is a 21-carbon steroid hormone.
  • HY-B0625
    Ciclesonide Agonist 98.95%
    Ciclesonide(RPR251526) is a glucocorticoid used to treat obstructive airway diseases.
  • HY-B0328
    Triamcinolone Inhibitor 99.15%
    Triamcinolone is a long-acting synthetic corticosteroid.
  • HY-B0154
    Fluticasone (propionate) Agonist 99.97%
    Fluticasone propionate is a high affinity, selective GR (glucocorticoid receptor) agonist which is derived from fluticasone used to treat asthma and allergic rhinitis.
  • HY-N0835
    (20S)-Protopanaxatriol Agonist >98.0%
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
  • HY-13580
    Budesonide Agonist >98.0%
    Budesonide is a glucocortical steroid with potent anti-inflammatory activity.
  • HY-14648A
    Dexamethasone acetate Agonist
    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.
  • HY-13570
    Betamethasone Agonist 99.97%
    Betamethasone is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.
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