1. GPCR/G Protein
  2. 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 (50):

Cat. No. Product Name Effect Purity
  • HY-14648
    Dexamethasone Agonist 99.70%
    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 99.29%
    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-16722
    Fosdagrocorat Agonist
    Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
  • HY-16718
    Dagrocorat Agonist
    Dagrocorat is a novel and dissociated Glucocorticoid Receptor Agonist.
  • HY-109042
    Relacorilant Antagonist
    Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively; Relacorilant has entered phase 2 clinical study in patients with Cushing’s syndrome.
  • HY-B0214
    Prednisone Agonist 99.35%
    Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
  • HY-B1829A
    Dexamethasone phosphate disodium Agonist 99.68%
    Dexamethasone phosphate disodium 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-14648A
    Dexamethasone acetate Agonist 99.34%
    Dexamethasone acetate is a glucocorticoid receptor agonist.
  • HY-B0154
    Fluticasone propionate Agonist 99.57%
    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-B0260
    Methylprednisolone Agonist 99.67%
    Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.
  • HY-B0636
    Triamcinolone acetonide Agonist 99.08%
    Triamcinolone Acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone.
  • HY-14234
    Glucocorticoid receptor agonist Agonist 98.57%
    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
  • HY-15709
    AL 082D06 Antagonist 98.65%
    AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
  • HY-17461
    Cortisone Agonist 98.63%
    Cortisone is a 21-carbon steroid hormone. Cortisone is one of the main hormones released by the adrenal gland in response to stress.