1. Signaling Pathways
  2. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor

Glucocorticoid Receptor

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-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
  • HY-14648S
    Dexamethasone-d5
    Agonist 99.23%
    Dexamethasone-d5 is the 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>5</sub>
  • HY-13571AR
    Beclometasone dipropionate (Standard)
    Agonist
    Beclometasone dipropionate (Standard) is the analytical standard of Beclometasone dipropionate. This product is intended for research and analytical applications. Beclometasone dipropionate, the proagent of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate can be used for asthma .
    Beclometasone dipropionate (Standard)
  • HY-B1365
    Prednicarbate
    Agonist 99.81%
    Prednicarbate is a topical corticosteroid agent. Prednicarbate can be used for the research of inflammatory skin diseases, such as atopic dermatitis.
    Prednicarbate
  • HY-13570R
    Betamethasone (Standard)
    Agonist
    Betamethasone (Standard) is the analytical standard of Betamethasone. This product is intended for research and analytical applications. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.
    Betamethasone (Standard)
  • HY-N0583S5
    Hydrocortisone-d2
    Agonist 98.56%
    Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone-d<sub>2</sub>
  • HY-13693S
    Mometasone furoate-d3
    Agonist 98.80%
    Mometasone furoate-d3 is a deuterium labeled Mometasone furoate. Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity.
    Mometasone furoate-d<sub>3</sub>
  • 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-113364
    5α-Tetrahydrocorticosterone
    Agonist 99.87%
    5α-Tetrahydrocorticosterone (5α-HB), an endogenous steroid, is a glucocorticoid receptor (GR) agonist and a metabolite of Corticosterone (HY-B1618). 5α-Tetrahydrocorticosterone is an effective topical anti-inflammatory agent in vivo. 5α-Tetrahydrocorticosterone reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd of 268 nM. 5α-Tetrahydrocorticosterone can be used for research on inflammatory skin diseases.
    5α-Tetrahydrocorticosterone
  • HY-160178
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
    Agonist 99.72%
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal (Compound Preparation 8) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-3 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
  • HY-B1095
    Chlormadinone acetate
    Ligand 98.0%
    Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.
    Chlormadinone acetate
  • HY-B0636R
    Triamcinolone acetonide (Standard)
    Agonist
    Triamcinolone acetonide (Standard) is the analytical standard of Triamcinolone acetonide. This product is intended for research and analytical applications.
    Triamcinolone acetonide (Standard)
  • HY-77839R
    Cortodoxone (Standard)
    Antagonist
    Cortodoxone (Standard) is the analytical standard of Cortodoxone. This product is intended for research and analytical applications. Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates T cell proliferation and activation.
    Cortodoxone (Standard)
  • HY-111186
    Flocoumafen
    99.35%
    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
  • HY-159695A
    IONIS-GCCRRx sodium
    Antagonist
    IONIS-GCCRRx (ISIS 426115) sodium, a glucocorticoid receptor antagonist, is a 2'-O-methoxyethyl (2'-MOE) antisense oligonucleotide (ASO).
    IONIS-GCCRRx sodium
  • HY-B0469S
    Medroxyprogesterone acetate-d3
    98.13%
    Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate-d<sub>3</sub>
  • HY-157294
    GSK866
    Agonist 98.0%
    GSK866 ((S)-GSK47866A) is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM.
    GSK866
  • HY-B0328R
    Triamcinolone (Standard)
    Inhibitor
    Triamcinolone (Standard) is the analytical standard of Triamcinolone. This product is intended for research and analytical applications.
    Triamcinolone (Standard)
  • HY-145351
    BAY 1003803
    Agonist 99.85%
    BAY 1003803 is a glucocorticoid receptor agonist for the topical research of psoriasis or severe atopic dermatitis.
    BAY 1003803
Cat. No. Product Name / Synonyms Application Reactivity