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-123352
    ZK 216348
    Agonist 98.59%
    ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.
    ZK 216348
  • HY-B1618R
    Corticosterone (Standard)
    Agonist
    Corticosterone (Standard) is the analytical standard of Corticosterone. This product is intended for research and analytical applications. Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect.
    Corticosterone (Standard)
  • HY-N0583S3
    Hydrocortisone-d3
    Agonist ≥98.0%
    Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
    Hydrocortisone-d<sub>3</sub>
  • HY-134116
    Isoflupredone acetate
    98.55%
    Isoflupredone acetate is a corticosteroids with anti-inflammatory activity. Isoflupredone acetate can be used for research ketosis, musculoskeletal disorders, hypersensitivity, infections, inflammatory diseases in cows, horse, pigs, et al..
    Isoflupredone acetate
  • HY-U00089
    Hydrocortisone cypionate
    Agonist 98.04%
    Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
    Hydrocortisone cypionate
  • HY-14648AR
    Dexamethasone acetate (Standard)
    Agonist 98.93%
    Dexamethasone acetate (Standard) is the analytical standard of Dexamethasone acetate. This product is intended for research and analytical applications. Dexamethasone acetate (Dexamethasone 21-acetate) 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 acetate (Standard)
  • HY-B1087
    Prednisolone hemisuccinate
    99.89%
    Prednisolone hemisuccinate is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
    Prednisolone hemisuccinate
  • HY-A0158
    Diflorasone
    Agonist 99.86%
    Diflorasone act as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties. Diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Diflorasone is used for the research of skin diseases such as eczema or psoriasis.
    Diflorasone
  • HY-12946
    BI 653048
    Inhibitor 99.84%
    BI 653048 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 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
  • HY-14648G
    Dexamethasone (GMP)
    Agonist
    Dexamethasone (Hexadecadrol) (GMP) is Dexamethasone (HY-14648) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dexamethasone is an agonist of glucocorticoid receptor.
    Dexamethasone (GMP)
  • HY-14648S3
    Dexamethasone-4,6α,21,21-d4
    Agonist ≥99.0%
    Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. 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-4,6α,21,21-d<sub>4</sub>
  • 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-113783
    Halobetasol
    99.10%
    Halobetasol (Ulobetasol) is a corticosteroid. Halobetasol can be used for research of severe localized psoriasis.
    Halobetasol
  • HY-B0625R
    Ciclesonide (Standard)
    Agonist 99.98%
    Ciclesonide (Standard) is the analytical standard of Ciclesonide. This product is intended for research and analytical applications. Ciclesonide (RPR251526) is a glucocorticoid with an potent anti-inflammatory activity. Ciclesonide can be used for asthma research.
    Ciclesonide (Standard)
  • 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[1].
    Mometasone furoate-d<sub>3</sub>
  • HY-107961
    Diflorasone diacetate
    99.86%
    Diflorasone diacetate is an anti-inflammatory steroid compound used as locally or topically agent. Diflorasone diacetate is being used for skin disorders to control corticosteroid-responsive dermatoses.
    Diflorasone diacetate
  • HY-14864A
    (S)-Mapracorat
    Inhibitor 99.85%
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
    (S)-Mapracorat
  • HY-16718A
    Dagrocorat hydrochloride
    Agonist 99.85%
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride 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 hydrochloride can be used for the research of rheumatoid arthritis.
    Dagrocorat hydrochloride
  • HY-146564A
    HP210
    Modulator 98.96%
    HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.
    HP210
  • HY-116691
    Hydrocortisone aceponate
    Agonist 99.43%
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a potent topical glucocorticoid. Hydrocortisone aceponate can be used for various dermatoses research.
    Hydrocortisone aceponate
Cat. No. Product Name / Synonyms Application Reactivity