1. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  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 (224):

Cat. No. Product Name Effect Purity
  • HY-B1618
    Corticosterone Agonist
    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[1][2][3][4].
  • HY-N0583
    Hydrocortisone Agonist 99.91%
    Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
  • 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[1][2][3][4].
  • 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[3].
  • 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[1].
  • HY-B1402A
    Hydrocortisone hemisuccinate hydrate Agonist
    Hydrocortisone hemisuccinate hydrate (5,6,7-Trihydroxyflavone hydrate), a physiological glucocorticoid, is an orally active steroidal anti-in ammatory agent (SAID). Hydrocortisone hemisuccinate hydrate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate hydrate can be used for the research of ulcerative colitis (UC).
  • HY-120016
    RU 43044 Antagonist
    RU 43044 is a glucocorticoid receptor antagonist. RU 43044 shows an antidepressant-like effect, probably via an inhibition of enhanced prefrontal dopaminergic neurotransmission in these mouse models[1].
  • HY-107461
    LY2623091 Antagonist
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors[1][2].
  • HY-13683S1
    Mifepristone-13C,d3 Antagonist
    Mifepristone-13C,d3 is the 13C- and deuterium labeled Mifepristone. 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[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-B0154S1
    Fluticasone propionate-d5 Agonist
    Fluticasone propionate-d5 is deuterium labeled Fluticasone (propionate). 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[1][2].
  • HY-13571AS1
    Beclometasone dipropionate-d10 Agonist
    Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
  • HY-17461A
    Cortisone acetate Agonist 99.63%
    Cortisone acetate (Cortisone 21-acetate), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acetate acts as an immunosuppressant and anti-inflammatory agent. Cortisone acetate can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations[1][3][4].
  • 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[1]
  • HY-B1155
    Hydrocortisone phosphate Agonist
    Hydrocortisone phosphate (Hydrocortisone 21-phosphate), a physiological glucocorticoid, and is an orally active steroidal anti-in ammatory agent (SAID). Hydrocortisone phosphate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone phosphate can be used for the research of ulcerative colitis (UC).
  • 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[1][2].
  • HY-U00298
    Amebucort Modulator
    Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
  • HY-157294
    GSK866 Agonist
    GSK866 is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM[1].
  • HY-132811
    Dazucorilant Modulator 98.91%
    Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders[1][2].
  • HY-B1121S
    Flunisolide-d6 Activator
    Flunisolide-d6 is the deuterium labeled Flunisolide. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
  • HY-B0629R
    Mometasone (Standard)
    Mometasone (Standard) is the analytical standard of Mometasone. This product is intended for research and analytical applications. Mometasone is an inhaled glucocorticoid. Mometasone can be used in mild asthma with a low sputum eosinophil level. Mometasone has the potential for the research of chronic hand eczema and rhinosinusitis[1][2].