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-B0636R
    Triamcinolone acetonide (Standard)
    Agonist
    Triamcinolone acetonide (Standard) is the analytical standard of Triamcinolone acetonide. This product is intended for research and analytical applications.
    Triamcinolone acetonide (Standard)
  • HY-15234S
    Fluticasone furoate-d3
    Activator
    Fluticasone furoate-d3 is deuterium labeled Fluticasone furoate. 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[1][2].
    Fluticasone furoate-d<sub>3</sub>
  • HY-107461
    LY2623091
    Antagonist
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors.
    LY2623091
  • HY-17461R
    Cortisone (Standard)
    Agonist
    Cortisone (Standard) is the analytical standard of Cortisone. This product is intended for research and analytical applications. 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.
    Cortisone (Standard)
  • HY-151963
    PPARγ/GR modulator 1
    Agonist
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.
    PPARγ/GR modulator 1
  • HY-A0150
    Alclometasone
    Agonist
    Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
    Alclometasone
  • HY-B0727R
    Betamethasone valerate (Standard)
    Agonist
    Betamethasone valerate (Standard) is the analytical standard of Betamethasone valerate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-100087
    Budesonide impurity C
    Agonist
    Budesonide impurity C is an impurity of Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist.
    Budesonide impurity C
  • HY-B0636S2
    Triamcinolone acetonide-d7-1
    Agonist
    Triamcinolone acetonide-d7-1 is deuterium labeled Triamcinolone acetonide.
    Triamcinolone acetonide-d<sub>7</sub>-1
  • HY-121859
    RU28362
    Agonist
    RU28362 is a potent and selective glucocorticoid agonist. RU28362 increases the Bnip3 mRNA levels in neurons. RU28362 inhibits adrenocorticotrophic hormone (ACTH) and corticosterone secretion. RU28362 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RU28362
  • HY-B1197R
    Amcinonide (Standard)
    Agonist
    Amcinonide (Standard) is the analytical standard of Amcinonide. This product is intended for research and analytical applications. 0
    Amcinonide (Standard)
  • 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[1][2].
    Fluticasone propionate-d<sub>3</sub>
  • HY-14648S1
    Dexamethasone-d5-1
    Agonist
    Dexamethasone-d5-1 is deuterium labeled Dexamethasone. 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>5</sub>-1
  • HY-163673
    Glucocorticoid receptor modulator 4
    Modulator
    Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models.
    Glucocorticoid receptor modulator 4
  • HY-B1183R
    Hydrocortisone acetate (Standard)
    Agonist
    Hydrocortisone acetate (Standard) is the analytical standard of Hydrocortisone acetate. This product is intended for research and analytical applications.
    Hydrocortisone acetate (Standard)
  • HY-13609S
    Deflazacort-d5
    Agonist
    Deflazacort-d5 is the deuterium labeled Deflazacort. Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant[1].
    Deflazacort-d<sub>5</sub>
  • HY-13609R
    Deflazacort (Standard)
    Agonist
    Deflazacort (Standard) is the analytical standard of Deflazacort. This product is intended for research and analytical applications. Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant.
    Deflazacort (Standard)
  • 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-157294A
    (R)-GSK866
    Agonist
    (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-13683S2
    Mifepristone-d6
    Antagonist
    Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). 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.
    Mifepristone-d<sub>6</sub>
Cat. No. Product Name / Synonyms Application Reactivity