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-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-B1087
    Prednisolone hemisuccinate
    		99.34%
    Prednisolone hemisuccinate is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
    Prednisolone hemisuccinate
  • 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-B0328R
    Triamcinolone (Standard)
    		Inhibitor 98.42%
    Triamcinolone (Standard) is the analytical standard of Triamcinolone. This product is intended for research and analytical applications.
    Triamcinolone (Standard)
  • HY-145351
    BAY 1003803
    		Agonist 99.85%
    BAY 1003803 is a glucocorticoid receptor agonist for the topical research of psoriasis or severe atopic dermatitis.
    BAY 1003803
  • HY-14864A
    (S)-Mapracorat
    		Inhibitor 99.85%
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
    (S)-Mapracorat
  • HY-14648AR
    Dexamethasone acetate (Standard)
    		Agonist 98.93%
    Dexamethasone acetate (Standard) is the analytical standard of Dexamethasone acetate. This product is intended for research and analytical applications. Dexamethasone acetate (Dexamethasone 21-acetate) 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 acetate (Standard)
  • 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-U00098
    Prednisolone Tebutate
    		Modulator 99.82%
    Prednisolone tebutate is a synthetic glucocorticoid used as an antiinflammatory and immunosuppressant.
    Prednisolone Tebutate
  • 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-12946
    BI 653048
    		Inhibitor 99.84%
    BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048
  • HY-157294
    GSK866
    		Agonist ≥98.0%
    GSK866 is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM.
    GSK866
  • HY-163340
    GA32
    		Inhibitor 99.67%
    GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.
    GA32
  • HY-B0625R
    Ciclesonide (Standard)
    		Agonist 99.98%
    Ciclesonide (Standard) is the analytical standard of Ciclesonide. This product is intended for research and analytical applications. Ciclesonide (RPR251526) is a glucocorticoid with an potent anti-inflammatory activity. Ciclesonide can be used for asthma research.
    Ciclesonide (Standard)
  • HY-16718A
    Dagrocorat hydrochloride
    		Agonist 99.85%
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride 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 hydrochloride can be used for the research of rheumatoid arthritis.
    Dagrocorat hydrochloride
  • HY-146564A
    HP210
    		Modulator 98.96%
    HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.
    HP210
  • 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-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-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-160177
    Glucocorticoid receptor agonist-3
    		Agonist 98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
Cat. No. Product Name / Synonyms Application Reactivity