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-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[1].
    Prednisone acetate-d<sub>3</sub>
  • HY-14648S5
    Dexamethasone-d3-1
    Agonist 98.02%
    Dexamethasone-d3-1 (Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). 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>3</sub>-1
  • HY-100085S
    21-Desacetyldeflazacort-d5
    Agonist 99.34%
    21-Desacetyldeflazacort-d5 is the deuterium labeled 21-Desacetyldeflazacort[1].
    21-Desacetyldeflazacort-d<sub>5</sub>
  • HY-125096
    C108297
    Modulator 99.97%
    C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation.
    C108297
  • 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[1].
    Ciclesonide-d<sub>7</sub>
  • HY-159695
    IONIS-GCCRRx
    Antagonist
    IONIS-GCCRRx (ISIS 426115), a glucocorticoid receptor antagonist, is a 2'-O-methoxyethyl (2'-MOE) antisense oligonucleotide (ASO).
    IONIS-GCCRRx
  • HY-136340
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
    Agonist 99.93%
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione is an intermediate of delta 9,11 steroids synthesis, for example, Vamorolone (HY-109017). The delta 9,11 steroids are modifications of glucocorticoids and has anti-inflammatory properties. The delta 9,11 steroids are agents for protection against cell damage (lipid peroxidation) and inhibition of neovascularization.
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
  • HY-160178
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
    Agonist 99.72%
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal (Compound Preparation 8) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-3 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
  • HY-U00098
    Prednisolone Tebutate
    Modulator 99.82%
    Prednisolone tebutate is a synthetic glucocorticoid used as an antiinflammatory and immunosuppressant.
    Prednisolone Tebutate
  • HY-107939
    Paramethasone Acetate
    ≥98.0%
    Paramethasone acetate is a synthetic glucocorticoid, and shows anti-inflammatory and immunosuppressant activities.
    Paramethasone Acetate
  • HY-U00298
    Amebucort
    Modulator ≥99.0%
    Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
    Amebucort
  • 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-111186
    Flocoumafen
    99.17%
    Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.
    Flocoumafen
  • HY-B1829AR
    Dexamethasone phosphate (disodium) (Standard)
    Agonist
    Dexamethasone phosphate (disodium) (Standard) is the analytical standard of Dexamethasone phosphate (disodium). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is an orally active Glucocorticoid receptor agonist.
    Dexamethasone phosphate (disodium) (Standard)
  • 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-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-139556
    Zavacorilant
    Modulator
    Zavacorilant is capable of modulating glucocorticoid receptor (GR).
    Zavacorilant
  • HY-125839
    OP-3633
    Antagonist
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism.
    OP-3633
  • HY-13683S1
    Mifepristone-13C,d3
    Antagonist
    Mifepristone-13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mifepristone-<sup>13</sup>C,d<sub>3</sub>
  • 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[1][2].
    Fluticasone propionate-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity