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-157294A
    (R)-GSK866
    		Agonist 98.0%
    (R)-GSK866 ((R)-GSK47866A) 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-B0260S4
    Methylprednisolone-d2
    		Agonist 99.11%
    Methylprednisolone-d2 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>2</sub>
  • HY-B1900R
    Methylprednisolone succinate (Standard)
    		Agonist
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate (HY-B1900). This product is intended for research and analytical applications. Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.
    Methylprednisolone succinate (Standard)
  • HY-B0485R
    Fluocinonide (Standard)
    		Agonist
    Fluocinonide (Standard) is the analytical standard of Fluocinonide (HY-B0485). This product is intended for research and analytical applications. Fluocinonide is a glucocorticoid with anti-inflammatory and vasoconstrictor properties. Fluocinonide can be used for the research of oral vesiculoerosive diseases and inflammatory dermatoses.
    Fluocinonide (Standard)
  • 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-N0583S3
    Hydrocortisone-d3
    		Agonist 98.41%
    Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone-d<sub>3</sub>
  • HY-134116
    Isoflupredone acetate
    		98.55%
    Isoflupredone acetate is a corticosteroids with anti-inflammatory activity. Isoflupredone acetate can be used for research ketosis, musculoskeletal disorders, hypersensitivity, infections, inflammatory diseases in cows, horse, pigs, et al..
    Isoflupredone acetate
  • HY-B1893R
    Fluorometholone (Standard)
    		Agonist
    Fluorometholone (Standard) is the analytical standard of Fluorometholone. This product is intended for research and analytical applications. Fluorometholone, a synthetic glucocorticoid, is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic properties. Fluorometholone can be used for the research of dry eye.
    Fluorometholone (Standard)
  • HY-77839S
    Cortodoxone-d5
    		Agonist 99.90%
    Cortodoxone-d5 is the deuterium labeled Cortodoxone.
    Cortodoxone-d<sub>5</sub>
  • HY-129630S
    Tetrahydrocortisol-d5
    		Control 99.51%
    Tetrahydrocortisol-d5 is the deuterium labeled Tetrahydrocortisol. Tetrahydrocortisol is a metabolite of Hydrocortisone (HY-N0583) that fails to activate glucocorticoid receptor. Tetrahydrocortisol inhibits Dexamethasone (HY-14648)-induced formation of cross-linked actin networks. Tetrahydrocortisol acts as a synergist to enhance the activity of anticancer agents. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, ocular hypertension, lung cancer and breast cancer.
    Tetrahydrocortisol-d<sub>5</sub>
  • HY-14864A
    (S)-Mapracorat
    		Inhibitor 99.14%
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
    (S)-Mapracorat
  • 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-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).
    Cortodoxone-d<sub>2</sub>
  • HY-B0214S
    Prednisone-d8
    		Agonist 98.00%
    Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
    Prednisone-d<sub>8</sub>
  • 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-164893
    ABBV-154
    ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica.
    ABBV-154
  • HY-A0288
    Loteprednol
    Loteprednol is a synthetic corticosteroid that belongs to a family of glucocorticoids. Loteprednol has anti-inflammatory, antiallergic and immunosuppressive activities. Loteprednol can be used to study eye inflammation.
    Loteprednol
  • HY-15234S
    Fluticasone furoate-d3
    		Activator 99.43%
    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.
    Fluticasone furoate-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.
    Fluticasone propionate-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity