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-B0214R
    Prednisone (Standard)
    		Agonist
    Prednisone (Standard) is the analytical standard of Prednisone. This product is intended for research and analytical applications. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.
    Prednisone (Standard)
  • HY-13580R
    Budesonide (Standard)
    		Agonist
    Budesonide (Standard) is the analytical standard of Budesonide. This product is intended for research and analytical applications. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
    Budesonide (Standard)
  • HY-17570
    Desoximetasone
    		98.72%
    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
  • HY-U00089
    Hydrocortisone cypionate
    		Agonist 99.73%
    Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
    Hydrocortisone cypionate
  • HY-103662
    GW-870086
    		Agonist 99.59%
    GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
    GW-870086
  • HY-164860
    Glucocorticoid receptor agonist-5
    		Agonist 99.95%
    Glucocorticoid receptor agonist-5 (compound 4), a glucocorticoid molecule, is a potent glucocorticoid receptor agonist. Glucocorticoid receptor agonist-5 shows anti-inflammatory and immunosuppressive activity. Glucocorticoid receptor agonist-5 is used as an ADC Cytotoxin for antibody-drug conjugate.
    Glucocorticoid receptor agonist-5
  • HY-B1087
    Prednisolone hemisuccinate
    		99.89%
    Prednisolone hemisuccinate (Prednisolone 21-hemisuccinate) is a prodrug of Prednisolone (HY-17463) and a glucocorticoid. Prednisolone hemisuccinate converts to Prednisolone in vivo. Prednisolone hemisuccinate induces the inactivation of glyceraldehyde-3-phosphate dehydrogenase (GAP-DH) in vitro. Prednisolone hemisuccinate can be used in research related to cataracts.
    Prednisolone hemisuccinate
  • HY-A0158
    Diflorasone
    		99.84%
    Diflorasone is a potent topical anti-inflammatory Corticosteroid. Diflorasone induces vasoconstriction when applied topically. Diflorasone can be used in research related to psoriasis, atopic dermatitis/neurodermatitis.
    Diflorasone
  • HY-13580S
    Budesonide-d8
    		Agonist 98.3%
    Budesonide-d8 is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
    Budesonide-d<sub>8</sub>
  • HY-B1618S1
    Corticosterone-d4
    		Agonist 99.17%
    Corticosterone-d4 is the deuterium labeled Corticosterone. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
    Corticosterone-d<sub>4</sub>
  • 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-16718
    Dagrocorat
    		Agonist 99.90%
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat 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 can be used for the research of rheumatoid arthritis.
    Dagrocorat
  • HY-163340
    GA32
    		Inhibitor 99.67%
    GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.
    GA32
  • HY-150701
    INCB13739
    		Inhibitor 99.79%
    INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.
    INCB13739
  • HY-113783
    Halobetasol
    		99.11%
    Halobetasol (Ulobetasol) is a corticosteroid. Halobetasol can be used for research of severe localized psoriasis.
    Halobetasol
  • HY-N0583S1
    Hydrocortisone-d7
    		Agonist 99.91%
    Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone-d<sub>7</sub>
  • HY-B1013
    Flurandrenolide
    		99.94%
    Fludroxycortide is a synthetic topical steroid with anti-inflammatory effects and has potential for use in skin irritation.
    Flurandrenolide
  • HY-132269
    Isoflupredone
    		Ligand 99.01%
    Isoflupredone belongs to the class of corticosteroids and exerts its effect by binding to glucocorticoid and mineralocorticoid receptors of animals, such as horses. Isoflupredone can be used in wide range of conditions, such as infection and inflammatory diseases.
    Isoflupredone
  • HY-164894
    ABBV-3373
    		98.78%
    ABBV-3373 is an anti-TNF antibody-drug conjugate (ADC). ABBV-3373 consists of a humanized TNF antibody Adalimumab (HY-P9908) conjugated to a glucocorticoid receptor agonist (HY-148436). ABBV-3373 can be used for the research of rheumatoid arthritis.
    ABBV-3373
  • HY-12946
    BI 653048
    		Inhibitor 99.84%
    BI 653048, a chemical probe, 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 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048
Cat. No. Product Name / Synonyms Application Reactivity