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 98.08%
    Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. Methylprednisolone succinate is the prodrug of methylprednisolone. Methylprednisolone succinate can be studied in liver diseases.
    Methylprednisolone succinate
  • HY-B1893
    Fluorometholone
    		Agonist 99.81%
    Fluorometholone, a synthetic glucocorticoid, is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic properties. Fluorometholone can be used for the research of dry eye.
    Fluorometholone
  • HY-13683R
    Mifepristone (Standard)
    		Antagonist
    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
    		99.82%
    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-15709
    AL 082D06
    		Antagonist 98.92%
    AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
    AL 082D06
  • 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-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-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-17463R
    Prednisolone (Standard)
    		Agonist
    Prednisolone (Standard) is the analytical standard of Prednisolone. This product is intended for research and analytical applications. Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
    Prednisolone (Standard)
  • 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-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-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-13571
    Betamethasone dipropionate
    		Modulator 99.40%
    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate
  • 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-103548
    GSK9027
    		Agonist 98.85%
    GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone.
    GSK9027
  • HY-B0260R
    Methylprednisolone (Standard)
    		Agonist
    Methylprednisolone (Standard) is the analytical standard of Methylprednisolone. This product is intended for research and analytical applications. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone (Standard)
  • 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-B1197
    Amcinonide
    		Agonist 99.61%
    Amcinonide is an inhibitor of NO release (IC50 = 3.38 nM). Amcinonide inhibits NNC-induced expression of the proinflammatory genes iNOS, TNF-α, and IL-1β in glial cells. Amcinonide reduces the numbers of T6+/Ia+ cells with a concomitant increase in T6+/Ia- cells. Amcinonide induces a selective reduction in expression of Ia antigens. Amcinonide can also be studied in research for eczematous dermatitis.
    Amcinonide
  • 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-B1076
    Medrysone
    		99.79%
    Medrysone is a corticosteroid with potential for research on ocular inflammation in ophthalmology.
    Medrysone
Cat. No. Product Name / Synonyms Application Reactivity