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-B1214
    Prednisolone acetate
    Agonist 99.83%
    Prednisolone acetate (Prednisolone 21-acetate) is an adrenocortical hormone active molecule with various pharmacological effects such as anti-inflammatory, anti-allergic, and immune suppression.
    Prednisolone acetate
  • HY-14930
    Mirodenafil
    Modulator 99.70%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
  • HY-153345
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
    Agonist 99.67%
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br is an Drug-linker conjugates for ADC that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs).
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
  • HY-131974
    Glucocorticoid receptor agonist-1
    Agonist 99.80%
    Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM extracted from patent WO2017210471A1, compound 41.
    Glucocorticoid receptor agonist-1
  • 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-113854
    AZD2906
    Agonist 99.68%
    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-13580R
    Budesonide (Standard)
    Agonist 99.78%
    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-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-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-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-17463R
    Prednisolone (Standard)
    Agonist 99.63%
    Prednisolone (Standard) is the analytical standard of Prednisolone. This product is intended for research and analytical applications. Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
    Prednisolone (Standard)
  • HY-B0260R
    Methylprednisolone (Standard)
    Agonist 99.67%
    Methylprednisolone (Standard) is the analytical standard of Methylprednisolone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-137882
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
    Agonist 99.94%
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC.
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
  • HY-B0629
    Mometasone
    99.13%
    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
  • HY-17461S1
    Cortisone-d8
    Agonist 98.17%
    Cortisone-d8 is the deuterium labeled Cortisone. 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[1][3][4].
    Cortisone-d<sub>8</sub>
  • HY-77839S
    Cortodoxone-d5
    Agonist 99.90%
    Cortodoxone-d5 is the deuterium labeled Cortodoxone.
    Cortodoxone-d<sub>5</sub>
  • HY-U00089
    Hydrocortisone cypionate
    Agonist 98.04%
    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-B0469R
    Medroxyprogesterone acetate (Standard)
    99.24%
    Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate (Standard)
  • HY-148435
    Glucocorticoid receptor agonist-2
    Agonist 99.65%
    Glucocorticoid receptor agonist-2 (compound 21) is an glucocorticoid receptor agonist with an IC50 value of 6.6 nM. Glucocorticoid receptor agonist-2 can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference of ABBV-3373.
    Glucocorticoid receptor agonist-2
Cat. No. Product Name / Synonyms Application Reactivity