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-123352A
    (-)-ZK 216348
    		Agonist 99.59%
    (-)-ZK 216348 is the enantiomer of (+)-ZK 216348 (HY-123352). (+)-ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.
    (-)-ZK 216348
  • HY-U00098
    Prednisolone Tebutate
    		Modulator 99.82%
    Prednisolone tebutate is a synthetic glucocorticoid used as an antiinflammatory and immunosuppressant.
    Prednisolone Tebutate
  • 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-B0260S3
    Methylprednisolone-d7
    		Agonist 99.73%
    Methylprednisolone-d7 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>7</sub>
  • HY-107939
    Paramethasone Acetate
    		98.0%
    Paramethasone Acetate is an orally active long-acting glucocorticoid. Paramethasone Acetate directly inhibits testicular aromatase, thereby reducing the synthesis of estradiol. Paramethasone Acetate suppresses the basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone Acetate also decreases circulating levels of dihydrotestosterone, androstenedione and estradiol in male animals. Paramethasone Acetate inhibits cartilage degeneration and alleviates joint pathological damage in osteoarthritis models. Paramethasone Acetate can be used in research related to osteoarthritis and endocrinology.
    Paramethasone Acetate
  • HY-B0154S
    Fluticasone propionate-d3
    		Agonist
    Fluticasone propionate-d3 is the 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.
    Fluticasone propionate-d<sub>3</sub>
  • HY-U00298
    Amebucort
    		Modulator 99.0%
    Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
    Amebucort
  • 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.
    Mometasone (Standard)
  • HY-B1829
    Dexamethasone phosphate
    		Agonist 98.89%
    Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate 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 inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
    Dexamethasone phosphate
  • HY-13693S2
    Mometasone furoate-13C,d6
    		Agonist 99.67%
    Mometasone furoate-13C,d6 (Sch32088-13C,d6) is 13C-labeled Mometasone furoate (HY-13693).
    Mometasone furoate-<sup>13</sup>C,d<sub>6</sub>
  • HY-W778340
    16α-Hydroxy-11-keto prednisolone
    		Control
    16α-Hydroxy-11-keto prednisolone (compound M-X) is a metabolite of Budesonide (HY-13580). Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide is a widely used for study of asthma, rhinitis, and inflammatory bowel disease.
    16α-Hydroxy-11-keto prednisolone
  • HY-W744549
    20β-Dihydrocortisol
    		Agonist
    20β-Dihydrocortisol (20β-DHF) is a metabolite of Hydrocortisone (Cortisol) (HY-N0583). 20β-Dihydrocortisol is a weak endogenous agonist of the glucocorticoid receptor (GR). 20β-Dihydrocortisol can be converted from Hydrocortisone via CBR1 catalysis, a process dependent on NADPH. 20β-Dihydrocortisol can be used for the study of obesity.
    20β-Dihydrocortisol
  • HY-B1832S
    Prednisone acetate-d3
    		Agonist
    Prednisone acetate-d3 is the deuterium labeled Prednisone acetate. Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties.
    Prednisone acetate-d<sub>3</sub>
  • HY-B1540R
    Beclometasone (Standard)
    		Agonist
    Beclometasone (Standard) is the analytical standard of Beclometasone. This product is intended for research and analytical applications. Beclometasone (Beclomethasone) is a prototype glucocorticoid receptor agonist.
    Beclometasone (Standard)
  • HY-137197
    6β-Hydroxy dexamethasone
    		Control 99.03%
    6β-Hydroxy dexamethasone is an active metabolite of the synthetic glucocorticoid Dexamethasone (HY-14648).
    6β-Hydroxy dexamethasone
  • HY-15234S1
    Fluticasone furoate-d5
    		Activator 99.65%
    Fluticasone furoate-d5 is deuterium-labeled Fluticasone furoate (HY-15234).
    Fluticasone furoate-d<sub>5</sub>
  • HY-W701984
    11β-Hydroxyetiocholanolone
    		Control
    11β-Hydroxyetiocholanolone is a metabolite of Hydrocortisone (HY-N0583). Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    11β-Hydroxyetiocholanolone
  • HY-B0645R
    Prednisolone disodium phosphate (Standard)
    		Agonist
    Prednisolone (disodium phosphate) (Standard) is the analytical standard of Prednisolone (disodium phosphate). This product is intended for research and analytical applications.
    Prednisolone disodium phosphate (Standard)
  • HY-15234R
    Fluticasone furoate (Standard)
    		Activator
    Fluticasone furoate (Standard) is the analytical standard of Fluticasone furoate. This product is intended for research and analytical applications. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
    Fluticasone furoate (Standard)
  • HY-B0260S6
    Methylprednisolone-d3-1
    Methylprednisolone-d3-1 (U 7532-d3-1) is the deuterium labeled Methylprednisolone (HY-B0260). Methylprednisolone (U 7532) 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>3</sub>-1
Cat. No. Product Name / Synonyms Application Reactivity