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-120273
    Glucocorticoids receptor agonist 3
    		Agonist
    Glucocorticoids receptor agonist 3 is a potent agonist of glucocorticoids receptor. Glucocorticoids receptor agonist 3 is useful to research diseases, such as obesity, diabetes, and inflammation (extracted from patent WO2000066522A1, compound 345).
    Glucocorticoids receptor agonist 3
  • HY-142941
    Glucocorticoid receptor-IN-1
    		Inhibitor
    Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV.
    Glucocorticoid receptor-IN-1
  • HY-164893
    ABBV-154
    ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica.
    ABBV-154
  • HY-B1829
    Dexamethasone phosphate
    		Agonist
    Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a biologically inactive compound which undergoes dephosphorylation by intra-erythrocyte enzymes. The active metabolite, Dexamethasone, is then released into the circulation by simple passive diffusion through cell membranes. Dexamethasone phosphate disodium-encapsulated erythrocyte has the potential for steroid-dependent ulcerative colitis research.
    Dexamethasone phosphate
  • HY-123163
    JNJ-1250132
    		Inhibitor
    JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM).
    JNJ-1250132
  • HY-B0260S4
    Methylprednisolone-d2
    		Agonist
    Methylprednisolone-d2 is the deuterium labeled Methylprednisolone. 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-d<sub>2</sub>
  • HY-134520R
    21-Deacetoxy deflazacort (Standard)
    21-Deacetoxy deflazacort (Standard) is the analytical standard of 21-Deacetoxy deflazacort. This product is intended for research and analytical applications. 21-Deacetoxy deflazacort is a dehydrogenated derivative of Deflazacort (HY-13609), a glucocorticoid, an inactive precursor that is rapidly converted to the active metabolite 21-Desacetyldeflazacort. Deflazacort acts as an anti-inflammatory and immunosuppressant.
    21-Deacetoxy deflazacort (Standard)
  • HY-149165
    Glucocorticoid receptor modulator 2
    		Modulator 99.84%
    Glucocorticoid receptor modulator 2 (Example 1) is a glucocorticoid receptor modulator, with an IC50 value less than 100 nM. Glucocorticoid receptor modulator 2 can be used for research of inflammatory and immune diseases.
    Glucocorticoid receptor modulator 2
  • HY-17461AR
    Cortisone acetate (Standard)
    		Agonist
    Cortisone acetate (Standard) is the analytical standard of Cortisone acetate. This product is intended for research and analytical applications. Cortisone acetate (Cortisone 21-acetate), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acetate acts as an immunosuppressant and anti-inflammatory agent. Cortisone acetate can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone acetate (Standard)
  • HY-142123
    Fluocortolone
    Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg).
    Fluocortolone
  • HY-119296R
    Cloprednol (Standard)
    Cloprednol (Standard) is the analytical standard of Cloprednol. This product is intended for research and analytical applications. Cloprednol is an orally active synthetic glucocorticoid. Cloprednol has anti-inflammatory activity, and can be used in the research of asthma.
    Cloprednol (Standard)
  • HY-13683S2
    Mifepristone-d6
    		Antagonist
    Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). 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-d<sub>6</sub>
  • HY-B1265
    Hydrocortisone 17-valerate
    		≥98.0%
    Hydrocortisone 17-valerate (Cortisol 17-valerate), a Hydrocortisone (HY-N0583) derivative, a corticosteroid ester. Hydrocortisone 17-valerate has anti-inflammatory effects.
    Hydrocortisone 17-valerate
  • HY-160182
    INX-P
    INX-P is glucocorticosteroid-target antibody drug conjugate (ADC).
    INX-P
  • HY-144397
    LEO 134310
    		Agonist
    LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases.
    LEO 134310
  • HY-117965
    Miricorilant
    		Modulator
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders.
    Miricorilant
  • HY-B0214R
    Prednisone (Standard)
    		Agonist
    Prednisone (Standard) is the analytical standard of Prednisone. This product is intended for research and analytical applications. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.
    Prednisone (Standard)
  • HY-134520
    21-Deacetoxy deflazacort
    21-Deacetoxy deflazacort is a dehydrogenated derivative of Deflazacort (HY-13609), a glucocorticoid, an inactive precursor that is rapidly converted to the active metabolite 21-Desacetyldeflazacort. Deflazacort acts as an anti-inflammatory and immunosuppressant.
    21-Deacetoxy deflazacort
  • HY-B1540S
    Beclomethasone-d5
    		Agonist
    Beclomethasone-d5 is the deuterium labeled Beclometasone. Beclometasone (Beclomethasone) is a prototype glucocorticoid receptor agonist.
    Beclomethasone-d<sub>5</sub>
  • HY-B0214S2
    Prednisone-d4
    		Agonist
    Prednisone-d4 is deuterated labeled Prednisone (HY-B0214). Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.
    Prednisone-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity