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-N0583S5
    Hydrocortisone-d2
    		Agonist
    Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1][2].
    Hydrocortisone-d<sub>2</sub>
  • HY-13571S1
    Betamethasone dipropionate-d5
    		Modulator
    Betamethasone dipropionate-d5 (Betamethasone 17,21-dipropionate-d5) is deuterium-labeled Betamethasone dipropionate (HY-13571).
    Betamethasone dipropionate-d5
  • HY-14648R
    Dexamethasone (Standard)
    		Agonist
    Dexamethasone (Standard) is the analytical standard of Dexamethasone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1540R
    Beclometasone (Standard)
    		Agonist
    Beclometasone (Standard) is the analytical standard of Beclometasone. This product is intended for research and analytical applications. Beclometasone (Beclomethasone) is a prototype glucocorticoid receptor agonist.
    Beclometasone (Standard)
  • HY-17358S1
    Loteprednol Etabonate-d3
    		Agonist
    Loteprednol Etabonate-d3 is the deuterium labeled Loteprednol Etabonate. Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology[1][2][3].
    Loteprednol Etabonate-d<sub>3</sub>
  • HY-13571AS
    Beclometasone dipropionate-d6
    		Agonist
    Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
    Beclometasone dipropionate-d<sub>6</sub>
  • HY-120492
    RS-21314
    RS-21314 is a thiol ester corticosteroid with anti-inflammatory effects.
    RS-21314
  • HY-125265
    JTP-117968
    		Modulator
    JTP-117968, a novel selective glucocorticoid receptor modulator (a non-steroidal SGRM, IC50 of 6.8 nM), exhibits improved transrepression/transactivation dissociation.
    JTP-117968
  • HY-111490R
    Desisobutyryl-ciclesonide (Standard)
    		Modulator
    Desisobutyryl-ciclesonide (Standard) is the analytical standard of Desisobutyryl-ciclesonide. This product is intended for research and analytical applications. Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.
    Desisobutyryl-ciclesonide (Standard)
  • HY-14648S2
    Dexamethasone-d4
    		Agonist
    Dexamethasone-d4 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>4</sub>
  • HY-13570CS
    Betamethasone 21-phosphate-d5
    Betamethasone 21-phosphate-d5 is the deuterium labeled Betamethasone disodium phosphate. Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a kind of corticosteroid, which is commonly used in the intralesional research of keloids[1].
    Betamethasone 21-phosphate-d<sub>5</sub>
  • HY-B1893R
    Fluorometholone (Standard)
    		Agonist 99.94%
    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-139710
    Glucocorticoids receptor agonist 2
    		Agonist
    Glucocorticoids receptor agonist 2 is a potent anti-inflammatory, arylpyrazole-based glucocorticoid receptor agonist that does not impair insulin secretion.
    Glucocorticoids receptor agonist 2
  • HY-13681R
    Methylprednisolone acetate (Standard)
    		Agonist
    Methylprednisolone acetate (Standard) is the analytical standard of Methylprednisolone acetate. This product is intended for research and analytical applications. Methylprednisolone acetate, a prednisolone derivative, is a corticosteroid hormone. Methylprednisolone acetate can relieve pain and swelling that occurs with arthritis and other joint disorders in vivo.
    Methylprednisolone acetate (Standard)
  • 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-159695
    IONIS-GCCRRx
    		Antagonist
    IONIS-GCCRRx (ISIS 426115), a glucocorticoid receptor antagonist, is a 2'-O-methoxyethyl (2'-MOE) antisense oligonucleotide (ASO).
    IONIS-GCCRRx
  • HY-136340
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
    		Agonist 99.84%
    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-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
Cat. No. Product Name / Synonyms Application Reactivity