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-116691
    Hydrocortisone aceponate
    Agonist 99.43%
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a potent topical glucocorticoid. Hydrocortisone aceponate can be used for various dermatoses research.
    Hydrocortisone aceponate
  • HY-77839S1
    Cortodoxone-d2
    Agonist 99.00%
    Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone)[1].
    Cortodoxone-d<sub>2</sub>
  • HY-123352A
    (-)-ZK 216348
    Agonist 98.92%
    (-)-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-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-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[3].
    Methylprednisolone-d<sub>7</sub>
  • HY-13580S
    Budesonide-d8
    Agonist
    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[1][2][3].
    Budesonide-d<sub>8</sub>
  • HY-157294A
    (R)-GSK866
    Agonist ≥98.0%
    (R)-GSK866 is the (R)-enantiomer of GSK866 (HY-157294). GSK866 is a selective agonist for glucocorticoid receptor with an IC50 of 4.6 nM.
    (R)-GSK866
  • 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-B0469S
    Medroxyprogesterone acetate-d3
    98.13%
    Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
    Medroxyprogesterone acetate-d<sub>3</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-159695A
    IONIS-GCCRRx sodium
    Antagonist
    IONIS-GCCRRx (ISIS 426115) sodium, a glucocorticoid receptor antagonist, is a 2'-O-methoxyethyl (2'-MOE) antisense oligonucleotide (ASO).
    IONIS-GCCRRx sodium
  • 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-B1900R
    Methylprednisolone succinate (Standard)
    Agonist 99.73%
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate. This product is intended for research and analytical applications. Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
    Methylprednisolone succinate (Standard)
  • HY-N0583S1
    Hydrocortisone-d7
    Agonist
    Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
    Hydrocortisone-d<sub>7</sub>
  • HY-B0485R
    Fluocinonide (Standard)
    Agonist 99.16%
    Fluocinonide (Standard) is the analytical standard of Fluocinonide. This product is intended for research and analytical applications.
    Fluocinonide (Standard)
  • HY-151876
    Glucocorticoid receptor modulator 1
    Modulator 99.79%
    Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
    Glucocorticoid receptor modulator 1
  • 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
Cat. No. Product Name / Synonyms Application Reactivity