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-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-107949
    Flumethasone pivalate
    		Ligand 98.17%
    Flumethasone pivalate is a glucocorticoid corticosteroid and a corticosteroid ester. Flumetasone pivalate has anti-inflammatory, antipruritic, and vasoconstrictive activities.
    Flumethasone pivalate
  • HY-121062
    Betamethasone acibutate
    		Modulator
    Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.
    Betamethasone acibutate
  • HY-W777281
    Fluocinolone acetonide-13C3
    Fluocinolone acetonide-13C3 is the 13C-labeled Fluocinolone (Acetonide) (HY-B0415). Fluocinolone is a glucocorticoid glucocorticoid receptor agonist. Fluocinolone is effective in preventing both lipid accumulation and inflammation. Fluocinolone can promote the proliferation of DPCs and has the potential role in repairing injured pulp tissues. Fluocinolone can be used to study the prevention of chemotherapy-induced peripheral neuropathy caused by Paclitaxel (HY-B0015).
    Fluocinolone acetonide-<sup>13</sup>C<sub>3</sub>
  • HY-W744577
    Dexamethasone acetate-d5
    Dexamethasone acetate-d5 (Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5) is the deuterium labeled Dexamethasone acetate (HY-14648A). 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-d<sub>5</sub>
  • 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.
    Methylprednisolone-d<sub>4</sub>
  • 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.
    Betamethasone-d<sub>5</sub>-1
  • HY-13609S3
    Deflazacort-d3-1
    Deflazacort-d3-1 is the deuterium labeled Deflazacort (HY-13609). Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant.
    Deflazacort-d<sub>3</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.
    Cortisone-<sup>13</sup>C<sub>3</sub>
  • HY-B0636S1
    Triamcinolone acetonide-13C3
    Triamcinolone acetonide-13C3 is the 13C-labeled Triamcinolone acetonide (HY-B0636). 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-<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.
    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-W653985
    Cortodoxone-d7
    Cortodoxone-d7 (11-Deoxycortisol-d7) is a deuterium labeled Cortodoxone (HY-77839). Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates T cell proliferation and activation.
    Cortodoxone-d<sub>7</sub>
  • HY-B0629S
    Mometasone-d5
    Mometasone-d5 is the deuterium labeled Mometasone.
    Mometasone-d<sub>5</sub>
  • HY-176298
    Tegacorat
    		Agonist
    Tegacorat (Compound 447) is a glucocorticoid receptor agonist with an EC50 ＜ 100 nM. Tegacorat can be used in the research of inflammatory diseases.
    Tegacorat
  • 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-123580
    RU26988
    		Agonist
    RU26988 is a highly specific glucocorticoid receptor agonist with a very low affinity for salocorticoid receptors.
    RU26988
  • 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.
    Betamethasone-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity