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 (57):

Cat. No. Product Name Effect Purity
  • HY-14648
    Dexamethasone Agonist 99.86%
    Dexamethasone is a glucocorticoid receptor agonist.
  • HY-N0583
    Hydrocortisone Agonist 99.66%
    Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
  • HY-13683
    Mifepristone Antagonist 98.17%
    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-17463
    Prednisolone Agonist >98.0%
    Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
  • HY-120012
    AZD9567 Modulator >99.0%
    AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
  • HY-113854
    AZD2906 Agonist 99.82%
    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively.
  • HY-117880
    Exicorilant Antagonist
    Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia.
  • HY-B1829A
    Dexamethasone phosphate disodium Agonist 99.68%
    Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.
  • HY-B0214
    Prednisone Agonist 99.35%
    Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
  • HY-B0260
    Methylprednisolone Agonist 99.67%
    Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.
  • HY-14648A
    Dexamethasone acetate Agonist
    Dexamethasone acetate is a glucocorticoid receptor agonist.
  • 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-17461
    Cortisone Agonist 99.90%
    Cortisone is a 21-carbon steroid hormone.
  • 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-B0328
    Triamcinolone Inhibitor 99.15%
    Triamcinolone is a long-acting synthetic corticosteroid.
  • HY-14864
    Mapracorat Agonist 99.40%
    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
  • HY-14234
    Glucocorticoid receptor agonist Agonist 98.57%
    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
  • HY-15709
    AL 082D06 Antagonist 98.92%
    AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
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