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-119705
    Prednival
    Prednival is a glucocorticoid. Prednival is used in studies of sustained-release ocular drug delivery.
    Prednival
  • 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-17570S
    Desoximetasone-d3
    Desoximetasone-d3 is the deuterium labeled Desoximetasone (HY-17570). 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-d<sub>3</sub>
  • HY-107122
    MK-5932
    		Agonist
    MK-5932 is an orally active, selective, dissociated partial glucocorticoid receptor agonist. MK-5932 inhibits IL-6. MK-5932 induces lymphopenia. MK-5932 restores glucose levels to normal. MK-5932 shows anti-inflammatory effects.
    MK-5932
  • HY-176877
    Glucocorticoid receptor/IL-6-IN-2
    		Inhibitor
    Glucocorticoid receptor/IL-6-IN-2 (Compound 36) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 40 nM and 19 nM, respectively). Glucocorticoid receptor/IL-6-IN-2 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma.
    Glucocorticoid receptor/IL-6-IN-2
  • 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-108061
    A-348441
    		Antagonist
    A-348441 is a liver selective glucocorticoid receptor antagonist. A-348441 can reduce the glucose level in the liver. A-348441 can be used for the research of metabolic disease, such as type 2 diabetes.
    A-348441
  • HY-13570B
    Betamethasone acetate
    		99.38%
    Betamethasone acetate is a glucocorticoid with prenatal application for preventing respiratory distress syndrome (RDS) in premature infants. Betamethasone acetate exhibits dose-dependent effects on somatic and brain development in offspring when administered prenatally to pregnant rats. Betamethasone acetate can be used for the study of antenatal intervention.
    Betamethasone acetate
  • HY-B0469S1
    Medroxyprogesterone acetate-d7
    Medroxyprogesterone acetate-d7 (Medroxyprogesterone 17-acetate-d7) is the deuterium labeled Medroxyprogesterone acetate (HY-B0469) . Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate-d<sub>7</sub>
  • HY-B1013R
    Flurandrenolide (Standard)
    Flurandrenolide (Fludroxycortide; Flurandrenolone) (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-176876
    Glucocorticoid receptor/IL-6-IN-1
    		Inhibitor
    Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 120 nM and 59 nM, respectively). Glucocorticoid receptor/IL-6-IN-1 inhibits IL-6-induced JAK/STAT3 phosphorylation, blocking inflammatory cytokine transcription. Glucocorticoid receptor/IL-6-IN-1 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma.
    Glucocorticoid receptor/IL-6-IN-1
  • 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-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-13571S2
    Betamethasone dipropionate-d6
    		Modulator
    Betamethasone dipropionate-d6 (Betamethasone 17,21-dipropionate-d6) is the deuterium labeled Betamethasone dipropionate (HY-13571). Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate-d<sub>6</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity