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-13570A
    Betamethasone hydrochloride
    		Agonist
    Betamethasone hydrochloride is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone hydrochloride accelerates fetal lung maturation and induces gene expression and apoptosis.
    Betamethasone hydrochloride
  • HY-164794
    Pyridyl disulfide-Dexamethasone
    		Agonist
    Pyridyl disulfide-Dexamethasone is a Dexamethasone (HY-14648) modified with pyridyl disulfide, which can be used for the synthesis of targeted peptide steroid conjugates.
    Pyridyl disulfide-Dexamethasone
  • HY-B0154S1
    Fluticasone propionate-d5
    		Agonist
    Fluticasone propionate-d5 is 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>5</sub>
  • HY-160179
    Glucocorticoid receptor agonist-4
    		Agonist 99.80%
    Glucocorticoid receptor agonist-4 (Compound Preparation 5) is a glucocorticoid receptor agonist that can be conjugated to TNF-α antibodies for the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-4
  • HY-160177
    Glucocorticoid receptor agonist-3
    		Agonist 98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
  • HY-B0625R
    Ciclesonide (Standard)
    		Agonist
    Ciclesonide (Standard) is the analytical standard of Ciclesonide. This product is intended for research and analytical applications. Ciclesonide (RPR251526) is a glucocorticoid with an potent anti-inflammatory activity. Ciclesonide can be used for asthma research.
    Ciclesonide (Standard)
  • HY-100085S
    21-Desacetyldeflazacort-d5
    		Agonist 99.34%
    21-Desacetyldeflazacort-d5 is the deuterium labeled 21-Desacetyldeflazacort.
    21-Desacetyldeflazacort-d<sub>5</sub>
  • HY-16718A
    Dagrocorat hydrochloride
    		Agonist 99.85%
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride 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 hydrochloride can be used for the research of rheumatoid arthritis.
    Dagrocorat hydrochloride
  • HY-B0260S
    Methylprednisolone-d3
    		Agonist
    Methylprednisolone-d3 is the 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>3</sub>
  • HY-B0625S
    Ciclesonide-d7
    		Agonist 99.99%
    Ciclesonide-d7 is the deuterium labeled Ciclesonide. Ciclesonide (RPR251526) is a glucocorticoid with an potent anti-inflammatory activity. Ciclesonide can be used for asthma research.
    Ciclesonide-d<sub>7</sub>
  • 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-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-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-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-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-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)
Cat. No. Product Name / Synonyms Application Reactivity