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-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-B0727
    Betamethasone valerate
    		Agonist 99.81%
    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
  • HY-14234
    Glucocorticoid receptor agonist
    		Agonist 99.06%
    Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.
    Glucocorticoid receptor agonist
  • HY-B1616
    Clobetasone butyrate
    		Agonist 99.80%
    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
  • HY-B1829AR
    Dexamethasone phosphate disodium (Standard)
    		Agonist
    Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
    Dexamethasone phosphate disodium (Standard)
  • HY-113854
    AZD2906
    		Agonist 99.90%
    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively.
    AZD2906
  • HY-B0214R
    Prednisone (Standard)
    		Agonist
    Prednisone (Standard) is the analytical standard of Prednisone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13580R
    Budesonide (Standard)
    		Agonist
    Budesonide (Standard) is the analytical standard of Budesonide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-U00089
    Hydrocortisone cypionate
    		Agonist 99.73%
    Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
    Hydrocortisone cypionate
  • HY-103662
    GW-870086
    		Agonist 99.59%
    GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
    GW-870086
  • HY-164860
    Glucocorticoid receptor agonist-5
    		Agonist 99.95%
    Glucocorticoid receptor agonist-5 (compound 4), a glucocorticoid molecule, is a potent glucocorticoid receptor agonist. Glucocorticoid receptor agonist-5 shows anti-inflammatory and immunosuppressive activity. Glucocorticoid receptor agonist-5 is used as an ADC Cytotoxin for antibody-drug conjugate.
    Glucocorticoid receptor agonist-5
  • HY-13580S
    Budesonide-d8
    		Agonist 98.3%
    Budesonide-d8 is the deuterium labeled Budesonide. 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-d<sub>8</sub>
  • HY-B1618S1
    Corticosterone-d4
    		Agonist 99.17%
    Corticosterone-d4 is the deuterium labeled Corticosterone. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
    Corticosterone-d<sub>4</sub>
  • HY-152121
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
    		Agonist
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody agent conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation.
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
  • HY-16718
    Dagrocorat
    		Agonist 99.90%
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.
    Dagrocorat
  • HY-16722
    Fosdagrocorat
    		Agonist 98.70%
    Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
    Fosdagrocorat
  • HY-N0583S1
    Hydrocortisone-d7
    		Agonist 99.91%
    Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone-d<sub>7</sub>
  • HY-107949
    Flumethasone pivalate
    		Agonist 98.17%
    Flumethasone pivalate (Flumethasone 21-pivalate) is a glucocorticoid and a topical corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive actions. Flumethasone pivalate inhibits foreign body granuloma formation. Flumethasone pivalate can be used for the researches of dermatitis, eczema, and psoriasis.
    Flumethasone pivalate
  • HY-14648S
    Dexamethasone-d5
    		Agonist 99.23%
    Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) 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-d<sub>5</sub>
  • HY-13571AR
    Beclometasone dipropionate (Standard)
    		Agonist
    Beclometasone dipropionate (Standard) is the analytical standard of Beclometasone dipropionate. This product is intended for research and analytical applications. Beclometasone dipropionate, the proagent of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate can be used for asthma .
    Beclometasone dipropionate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity