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-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-N8550
    Cortolone
    Control
    Cortolone (α-Cortolone) is a metabolite of the glucocorticoid cortisol (Hydrocortisone (HY-N0583)). Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Cortolone
  • 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-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-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-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-164894
    ABBV-3373
    ABBV-3373 is an anti-TNF antibody drug conjugate (ADC). ABBV-3373 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-148436). ABBV-3373 can be used in the study of rheumatoid arthritis.
    ABBV-3373
  • HY-B1121AR
    Flunisolide (hemihydrate) (Standard)
    Activator
    Flunisolide (hemihydrate) (Standard) is the analytical standard of Flunisolide (hemihydrate). This product is intended for research and analytical applications. 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) (Standard)
  • 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)
  • HY-B1832R
    Prednisone acetate (Standard)
    Agonist
    Prednisone acetate (Standard) is the analytical standard of Prednisone acetate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0636R
    Triamcinolone acetonide (Standard)
    Agonist
    Triamcinolone acetonide (Standard) is the analytical standard of Triamcinolone acetonide. This product is intended for research and analytical applications.
    Triamcinolone acetonide (Standard)
  • HY-106567
    Fluocortin butyl ester
    Activator
    Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when it is used topically. Fluocortin butyl ester appears to be an effective well-tolerated topical steroid useful in the research of perennial rhinitis.
    Fluocortin butyl ester
  • 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.
    LY2623091
  • HY-17461R
    Cortisone (Standard)
    Agonist
    Cortisone (Standard) is the analytical standard of Cortisone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-151963
    PPARγ/GR modulator 1
    Agonist
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.
    PPARγ/GR modulator 1
  • HY-A0150
    Alclometasone
    Agonist
    Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic?dermatitis, eczema, psoriasis and allergic dermatitis.
    Alclometasone
  • HY-B0727R
    Betamethasone valerate (Standard)
    Agonist
    Betamethasone valerate (Standard) is the analytical standard of Betamethasone valerate. This product is intended for research and analytical applications. Betamethasone valerate (Betamethasone 17-valerate), the 17-valerate ester of Betamethasone, is a topical corticosteroid with anti-inflammatory activity. Betamethasone valerate is used in the treatment of recurrent aphthous stomatitis. Betamethasone valerate inhibits the binding of the radiolabeled glucocorticoid dexamethasone (3H dexamethasone) to human epidermis and mouse skin with IC50s of 5 and 6 nM, respectively.
    Betamethasone valerate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity