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-14234
    Glucocorticoid receptor agonist
    		Agonist 99.06%
    Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.
    Glucocorticoid receptor agonist
  • HY-B1402B
    Hydrocortisone hemisuccinate sodium
    		Inhibitor 99.66%
    Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC).
    Hydrocortisone hemisuccinate sodium
  • HY-112710
    ORIC-101
    		Antagonist 99.30%
    ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity. ORIC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ORIC-101
  • HY-109042
    Relacorilant
    		Antagonist 99.37%
    Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
    Relacorilant
  • 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-N0583S3
    Hydrocortisone-d3
    		Agonist ≥98.0%
    Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
    Hydrocortisone-d<sub>3</sub>
  • HY-14864A
    (S)-Mapracorat
    		Inhibitor 99.85%
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
    (S)-Mapracorat
  • HY-N0583S2
    Hydrocortisone-d4
    		Agonist ≥98.0%
    Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
    Hydrocortisone-d<sub>4</sub>
  • 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-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-15710
    Cort108297
    		Antagonist 99.44%
    Cort108297 is a specific glucocorticoid receptor (GR) antagonist. Cort108297 has a high affinity for GRs with a Ki of 0.45 nM.
    Cort108297
  • 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-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-14648S
    Dexamethasone-d5
    		Agonist 99.86%
    Dexamethasone-d5 is the 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[1][2].
    Dexamethasone-d<sub>5</sub>
  • HY-157294
    GSK866
    		Agonist ≥98.0%
    GSK866 is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM.
    GSK866
  • 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
Cat. No. Product Name / Synonyms Application Reactivity