2. Signaling Pathways
  3. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  4. Glucocorticoid Receptor

Glucocorticoid Receptor

Glucocorticoid Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14648
    Dexamethasone
    		Agonist 99.86%
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist, apoptosis inducer, and common disease inducer in experimental animals, constructing models of muscle atrophy, hypertension, and depression. Dexamethasone can inhibit the production of inflammatory miRNA-155 exosomes in macrophages and significantly reduce the expression of inflammatory factors in neutrophils and monocytes. Dexamethasone also has potential for use in COVID-19 research.
    Dexamethasone
  • HY-N0583
    Hydrocortisone
    		Agonist 99.91%
    Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone
  • HY-B1618
    Corticosterone
    		Agonist 99.70%
    Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect.
    Corticosterone
  • HY-13683
    Mifepristone
    		Antagonist 99.77%
    Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
    Mifepristone
  • HY-B0260
    Methylprednisolone
    		Agonist 99.75%
    Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone
  • HY-117880
    Exicorilant
    		Antagonist 98.28%
    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.
    Exicorilant
  • HY-109042
    Relacorilant
    		Antagonist 99.37%
    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 the potential for Cushing’s syndrome treatment.
    Relacorilant
  • HY-157294
    GSK866
    		Agonist
    GSK866 is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM.
    GSK866
  • HY-B0469
    Medroxyprogesterone acetate
    		99.88%
    Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate
  • HY-B1829A
    Dexamethasone phosphate disodium
    		Agonist 99.76%
    Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is an orally active Glucocorticoid receptor agonist.
    Dexamethasone phosphate disodium
  • HY-17463
    Prednisolone
    		Agonist 99.96%
    Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
    Prednisolone
  • HY-B0214
    Prednisone
    		Agonist 99.84%
    Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.
    Prednisone
  • HY-13580
    Budesonide
    		Agonist 99.73%
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
    Budesonide
  • HY-14648A
    Dexamethasone acetate
    		Agonist 99.69%
    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
    Dexamethasone acetate
  • HY-B0636
    Triamcinolone acetonide
    		Agonist 99.05%
    Triamcinolone acetonide inhibits basic fibroblast growth factor (bFGF) induced proliferation of retinal endothelial cells. Triamcinolone acetonide reduces chondrocyte viability and leads to cartilage destruction. Triamcinolone acetonide activates macrophage with anti-inflammatory characteristics. Triamcinolone acetonide can be used in the study of diseases such as atopic dermatitis.
    Triamcinolone acetonide
  • HY-13693
    Mometasone furoate
    		Agonist 99.86%
    Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity. Mometasone furoate acts as a corticosteroid agent and used for topical applications in chronic skin eczema and airway inflammation management of asthma in vivo
    Mometasone furoate
  • HY-17461
    Cortisone
    		Agonist 99.90%
    Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone
  • HY-B1121
    Flunisolide
    		Activator 99.95%
    Flunisolide is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide
  • HY-B1832
    Prednisone acetate
    		Agonist 99.71%
    Prednisone acetate (Prednisone 21-acetate), a glucocorticoid, is an orally active Notch inhibitor. Prednisone acetate has anti-inflammatory activity and can enhance the immune response.
    Prednisone acetate
  • HY-B0154
    Fluticasone (propionate)
    		Agonist 99.97%
    Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity.
    Fluticasone (propionate)
Cat. No. Product Name / Synonyms Application Reactivity