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-B1900
    Methylprednisolone succinate
    		Agonist 99.11%
    Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
    Methylprednisolone succinate
  • HY-B0645
    Prednisolone disodium phosphate
    		Agonist 99.79%
    Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Prednisolone disodium phosphate can be rapidly and completely hydrolyzed to Prednisolone in the plasma.
    Prednisolone disodium phosphate
  • HY-15234
    Fluticasone furoate
    		Activator 99.84%
    Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
    Fluticasone furoate
  • HY-B1618S
    Corticosterone-d8
    		Agonist 99.91%
    Corticosterone-d8 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>8</sub>
  • HY-120012
    Mizacorat
    		Modulator 99.71%
    Mizacorat (AZD9567; compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
    Mizacorat
  • HY-13571
    Betamethasone dipropionate
    		Modulator 99.54%
    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate
  • HY-13683R
    Mifepristone (Standard)
    		Antagonist 98.49%
    Mifepristone (Standard) is the analytical standard of Mifepristone. This product is intended for research and analytical applications. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
    Mifepristone (Standard)
  • HY-103025
    Methylprednisolone aceponate
    		99.44%
    Methylprednisolone aceponate (ZK 91588) is a glucocorticoid and anti-inflammatory agent with weak systemic effects. Methylprednisolone aceponate is a selective glucocorticoid receptor Ligand.Methylprednisolone aceponate can be used for research of eczema and other inflammatory skin disorders.
    Methylprednisolone aceponate
  • HY-13681
    Methylprednisolone acetate
    		Agonist
    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
  • HY-B1197
    Amcinonide
    		Agonist 99.63%
    Amcinonide is a NO inhibitor that inhibits NO release from activated microglia with IC50 of 3.38 nM. Amcinonide has glucocorticoid receptor affinity.
    Amcinonide
  • HY-117880
    Exicorilant
    		Antagonist 99.48%
    Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia.
    Exicorilant
  • HY-131974
    Glucocorticoid receptor agonist-1
    		Agonist 99.80%
    Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM extracted from patent WO2017210471A1, compound 41.
    Glucocorticoid receptor agonist-1
  • HY-B1402B
    Hydrocortisone hemisuccinate sodium
    		Inhibitor 99.66%
    Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC).
    Hydrocortisone hemisuccinate sodium
  • HY-B0248
    Desonide
    		Inhibitor 99.64%
    Desonide is a non-fluorinated corticosteroid anti-inflammatory agent that acts on the glucocorticoid receptor. Desonide can also specifically bind to the mutant huntingtin protein (mHTT), reducing the level and toxicity of mHTT. Desonide can be used in the research of Huntington's disease and inflammatory diseases such as atopic dermatitis.
    Desonide
  • HY-B1183
    Hydrocortisone acetate
    		Agonist 99.14%
    Hydrocortisone acetate (Hydrocortisone 21-acetate) is a corticosteroid used to reduce swelling, itching and pain caused by minor skin irritations or hemorrhoids.
    Hydrocortisone acetate
  • HY-14864
    Mapracorat
    		Agonist 99.40%
    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
    Mapracorat
  • HY-14930
    Mirodenafil
    		Modulator 99.70%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
  • HY-109042
    Relacorilant
    		Antagonist 99.12%
    Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
    Relacorilant
  • HY-153345
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
    		Agonist 99.67%
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br is an Drug-linker conjugates for ADC that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs).
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
  • HY-108243
    AZD5423
    		Modulator 99.85%
    AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
    AZD5423
Cat. No. Product Name / Synonyms Application Reactivity