1. Signaling Pathways
  2. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1402R
    Hydrocortisone hemisuccinate (Standard)
    Agonist
    Hydrocortisone hemisuccinate (Standard) is the analytical standard of Hydrocortisone hemisuccinate. This product is intended for research and analytical applications. Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, is an orally active steroidal anti-in ammatory agent (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC).
    Hydrocortisone hemisuccinate (Standard)
  • HY-114154
    AL-438
    Modulator
    AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity.
    AL-438
  • HY-12946A
    BI 653048 phosphate
    Inhibitor
    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate 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.
    BI 653048 phosphate
  • HY-B1087R
    Prednisolone hemisuccinate (Standard)
    Prednisolone (hemisuccinate) (Standard) is the analytical standard of Prednisolone (hemisuccinate). This product is intended for research and analytical applications.
    Prednisolone hemisuccinate (Standard)
  • HY-121062
    Betamethasone acibutate
    Modulator
    Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.
    Betamethasone acibutate
  • HY-142942
    Glucocorticoid receptor-IN-2
    Inhibitor
    Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV.
    Glucocorticoid receptor-IN-2
  • HY-B0260S2
    Methylprednisolone-d4
    Agonist
    Methylprednisolone-d4 is deuterium labeled Methylprednisolone. 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].
    Methylprednisolone-d<sub>4</sub>
  • HY-B1616R
    Clobetasone butyrate (Standard)
    Agonist
    Clobetasone butyrate (Standard) is the analytical standard of Clobetasone butyrate. This product is intended for research and analytical applications. Clobetasone butyrate is a synthetic glucocorticoid and has topical anti-inflammatory activity especially in skin. Clobetasone butyrate can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis and psoriasis.
    Clobetasone butyrate (Standard)
  • HY-13570S1
    Betamethasone-d5-1
    Agonist
    Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis[1][2][3][4].
    Betamethasone-d<sub>5</sub>-1
  • HY-17461S
    Cortisone-13C3
    Agonist
    Cortisone-13C3 is the 13C-labeled Cortisone. 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[1][3][4].
    Cortisone-<sup>13</sup>C<sub>3</sub>
  • HY-17461S3
    Cortisone-d2
    Agonist
    Cortisone-d2 is the deuterium labeled Cortisone. 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[1][3][4][5].
    Cortisone-d<sub>2</sub>
  • 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.
    RU 43044
  • HY-B1121A
    Flunisolide hemihydrate
    Activator
    Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate
  • HY-B0629S
    Mometasone-d5
    Mometasone-d5 is the deuterium labeled Mometasone[1].
    Mometasone-d<sub>5</sub>
  • HY-13570S
    Betamethasone-d5
    Agonist
    Betamethasone-d5 is the deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis[1][2][3][4].
    Betamethasone-d<sub>5</sub>
  • HY-B0214S
    Prednisone-d8
    Agonist
    Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
    Prednisone-d<sub>8</sub>
  • HY-B0636S3
    Triamcinolone acetonide-d6
    Agonist 98.04%
    Triamcinolone acetonide-d6 is deuterium labeled Triamcinolone acetonide.
    Triamcinolone acetonide-d<sub>6</sub>
  • HY-17463S
    Prednisolone-d8
    Agonist
    Prednisolone-d8 is the deuterium labeled Prednisolone. 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[1][2].
    Prednisolone-d<sub>8</sub>
  • HY-121131
    Deacylcortivazol
    Activator
    Deacylcortivazol, a potent glucocorticoid, is a glucocorticoid receptor (GR) activator.
    Deacylcortivazol
  • HY-13693R
    Mometasone furoate (Standard)
    Agonist
    Mometasone furoate (Standard) is the analytical standard of Mometasone furoate. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity