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-B1754
    Rimexolone
    Rimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation.
    Rimexolone
  • HY-125558
    PT150
    		Antagonist
    PT150 (ORG-34517) is a competitive and orally active glucocorticoid receptor antagonist. PT150 shows neuroprotective effects. PT150 has the potential for the research of Parkinson’s disease.
    PT150
  • HY-B0260S
    Methylprednisolone-d3
    		Agonist
    Methylprednisolone-d3 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[3].
    Methylprednisolone-d<sub>3</sub>
  • HY-161520
    Glucocorticoid receptor/NF-κB modulator-1
    		Modulator
    Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model.
    Glucocorticoid receptor/NF-κB modulator-1
  • HY-B1214R
    Prednisolone acetate (Standard)
    		Agonist
    Prednisolone acetate (Standard) is the analytical standard of Prednisolone acetate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-163672
    Glucocorticoid receptor modulator 3
    		Modulator
    Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases.
    Glucocorticoid receptor modulator 3
  • HY-B1402R
    Hydrocortisone hemisuccinate (Standard)
    		Agonist
    Hydrocortisone hemisuccinate (Standard) is the analytical standard of Hydrocortisone hemisuccinate. This product is intended for research and analytical applications. Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, is an orally active steroidal anti-in ammatory agent (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC).
    Hydrocortisone hemisuccinate (Standard)
  • HY-114154
    AL-438
    		Modulator
    AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity.
    AL-438
  • HY-12946A
    BI 653048 phosphate
    		Inhibitor
    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate 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 phosphate
  • HY-N8550
    Cortolone
    		Control
    Cortolone (α-Cortolone) is a metabolite of the glucocorticoid cortisol (Hydrocortisone (HY-N0583)). Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Cortolone
  • HY-107949
    Flumethasone pivalate
    		Ligand
    Flumethasone pivalate is a glucocorticoid corticosteroid and a corticosteroid ester. Flumetasone pivalate has anti-inflammatory, antipruritic, and vasoconstrictive activities.
    Flumethasone pivalate
  • HY-121062
    Betamethasone acibutate
    		Modulator
    Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.
    Betamethasone acibutate
  • HY-142942
    Glucocorticoid receptor-IN-2
    		Inhibitor
    Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV.
    Glucocorticoid receptor-IN-2
  • HY-B0260S2
    Methylprednisolone-d4
    		Agonist
    Methylprednisolone-d4 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>4</sub>
  • 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-13570S1
    Betamethasone-d5-1
    		Agonist
    Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis[1][2][3][4].
    Betamethasone-d<sub>5</sub>-1
  • HY-17461S
    Cortisone-13C3
    		Agonist
    Cortisone-13C3 is the 13C-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-<sup>13</sup>C<sub>3</sub>
  • HY-17461S3
    Cortisone-d2
    		Agonist
    Cortisone-d2 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][5].
    Cortisone-d<sub>2</sub>
  • HY-120016
    RU 43044
    		Antagonist
    RU 43044 is a glucocorticoid receptor antagonist. RU 43044 shows an antidepressant-like effect, probably via an inhibition of enhanced prefrontal dopaminergic neurotransmission in these mouse models.
    RU 43044
  • HY-B1121A
    Flunisolide hemihydrate
    		Activator
    Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate
Cat. No. Product Name / Synonyms Application Reactivity