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-13681
    Methylprednisolone acetate
    		Agonist 99.95%
    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-B1214
    Prednisolone acetate
    		Agonist 99.83%
    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
  • HY-B1051
    Flumethasone
    		Agonist 99.84%
    Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation.
    Flumethasone
  • 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-136642
    Fluocinolone
    		Agonist 99.66%
    Fluocinolone is a corticosteroid that is used to relieve redness, itching, swelling, or other discomfort caused by skin conditions.
    Fluocinolone
  • 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
  • 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-B0469R
    Medroxyprogesterone acetate (Standard)
    Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate (Standard)
  • HY-14930
    Mirodenafil
    		Modulator 99.88%
    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-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-137882
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
    		Agonist 99.94%
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC.
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
  • HY-111453
    Velsecorat
    		Modulator 99.83%
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
    Velsecorat
  • HY-136239
    Beclomethasone 17-propionate
    		Agonist 99.76%
    Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages.
    Beclomethasone 17-propionate
  • HY-B0485
    Fluocinonide
    		Agonist 99.63%
    Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.
    Fluocinonide
  • 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-16722
    Fosdagrocorat
    		Agonist 98.70%
    Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
    Fosdagrocorat
  • HY-B0603
    Fluticasone
    		Agonist 98.70%
    Fluticasone is an inhaled corticosteroid used for respiratory research. Fluticasone is a Smo agonist with an IC50 value of 99 nM. Fluticasone activates Hedgehog signaling and promotes the proliferation of primary neuronal stem or precursor cells.
    Fluticasone
  • HY-113854
    AZD2906
    		Agonist 99.90%
    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively.
    AZD2906
  • 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-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)
Cat. No. Product Name / Synonyms Application Reactivity