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-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 98.93%
    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-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-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-13570B
    Betamethasone acetate
    		99.38%
    Betamethasone acetate is a glucocorticoid corticosteroid. Betamethasone acetate induces fetal lung maturation in preterm sheep.
    Betamethasone acetate
  • HY-B1013R
    Flurandrenolide (Standard)
    Flurandrenolide (Standard) is the analytical standard of Flurandrenolide. This product is intended for research and analytical applications.
    Flurandrenolide (Standard)
  • HY-P4407
    (D-Asn28)-Exenatide
    		Control
    (D-Asn28)-Exenatide is an Exenatide (HY-13443) impurity. Exenatide is a long-acting glucagon-like peptide-1 receptor agonist.
    (D-Asn28)-Exenatide
  • 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-111186R
    Flocoumafen (Standard)
    Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.
    Flocoumafen (Standard)
  • HY-17570R
    Desoximetasone (Standard)
    Desoximetasone (Standard) is the analytical standard of Desoximetasone (HY-17570). This product is intended for research and analytical applications. Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.
    Desoximetasone (Standard)
  • 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.
    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-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
Cat. No. Product Name / Synonyms Application Reactivity