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-176298
    Tegacorat
    		Agonist
    Tegacorat (Compound 447) is a glucocorticoid receptor agonist with an EC50 ＜ 100 nM. Tegacorat can be used in the research of inflammatory diseases.
    Tegacorat
  • HY-B1121AR
    Flunisolide hemihydrate (Standard)
    		Activator
    Flunisolide (hemihydrate) (Standard) is the analytical standard of Flunisolide (hemihydrate). This product is intended for research and analytical applications. Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate (Standard)
  • HY-123580
    RU26988
    		Agonist
    RU26988 is a highly specific glucocorticoid receptor agonist with a very low affinity for salocorticoid receptors.
    RU26988
  • HY-13570S
    Betamethasone-d5
    		Agonist
    Betamethasone-d5 is the deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.
    Betamethasone-d<sub>5</sub>
  • HY-181014
    Glucocorticoid receptor modulator 5
    		Modulator
    Glucocorticoid receptor modulator 5 (Compound D8) is a selective, orally active Glucocorticoid receptor modulator. Glucocorticoid receptor modulator 5 shows extremely high transrepression activity (TRNF-κB IC50 = 0.0009 μM, TRAP-1 IC50 = 0.0005 μM). Glucocorticoid receptor modulator 5 exerts its anti-inflammatory activity by interacting directly with the Glucocorticoid receptor signaling pathway. Glucocorticoid receptor modulator 5 significantly alleviates dermatitis and autoimmune hepatitis.
    Glucocorticoid receptor modulator 5
  • HY-117847
    LLY-2707
    		Antagonist
    LLY-2707 is a selective glucocorticoid receptor (GR) antagonist. LLY-2707 is promising for research of diabetes and psychiatric disorders such as schizophrenia.
    LLY-2707
  • HY-17463S
    Prednisolone-d8
    		Agonist
    Prednisolone-d8 is the deuterium labeled Prednisolone. 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-d<sub>8</sub>
  • HY-121131
    Deacylcortivazol
    		Activator
    Deacylcortivazol, a potent glucocorticoid, is a glucocorticoid receptor (GR) activator.
    Deacylcortivazol
  • HY-13570CR
    Betamethasone disodium phosphate (Standard)
    		Agonist
    Betamethasone disodium phosphate (Standard) is the analytical standard of Betamethasone disodium phosphate. This product is intended for research and analytical applications. Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a kind of corticosteroid, which is commonly used in the intralesional research of keloids.
    Betamethasone disodium phosphate (Standard)
  • HY-17461S4
    Cortisone-d9
    		Agonist
    Cortisone-d9 (17-Hydroxy-11-dehydrocorticosterone-d9) is the deuterium labeled Cortisone (HY-17461). Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone-d<sub>9</sub>
  • HY-B1832R
    Prednisone acetate (Standard)
    		Agonist
    Prednisone acetate (Standard) is the analytical standard of Prednisone acetate. This product is intended for research and analytical applications. Prednisone acetate (Prednisone 21-acetate), a glucocorticoid, is an orally active Notch inhibitor. Prednisone acetate has anti-inflammatory activity and can enhance the immune response.
    Prednisone acetate (Standard)
  • HY-106365
    Rofleponide
    Rofleponide is a synthetic glucocorticoid that has a high affinity for rat thymic glucocorticoid receptors and has high anti-inflammatory efficacy in experimental animal models.
    Rofleponide
  • HY-W424539
    Prednisolone sodium succinate
    Prednisolone (sodium succinate) is an anti-inflammatory corticosteroid and a prodrug of the glucocorticoid prednisolone. Prednisolone (sodium succinate) is used as an immunosuppressant.
    Prednisolone sodium succinate
  • HY-109026
    Benzodrocortisone
    		Agonist
    Benzodrocortisone is a glucocorticoid receptor agonist. Benzodrocortisone can be used in research on eye diseases.
    Benzodrocortisone
  • HY-106567
    Fluocortin butyl ester
    		Activator
    Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when it is used topically. Fluocortin butyl ester appears to be an effective well-tolerated topical steroid useful in the research of perennial rhinitis.
    Fluocortin butyl ester
  • HY-13571S3
    Betamethasone dipropionate-d6-1
    Betamethasone dipropionate-d6-1 (Betamethasone 17,21-dipropionate-d6-1) is the deuterium labeled Betamethasone dipropionate (HY-13571). Betamethasone dipropionate is a?glucocorticoid?steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate-d<sub>6</sub>-1
  • HY-W752724
    Flunisolide-d4
    Flunisolide-d4 is the deuterium labeled Flunisolide (HY-B1121). Flunisolide is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide-d<sub>4</sub>
  • HY-107461
    LY2623091
    		Antagonist
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors.
    LY2623091
  • HY-A0179
    Paramethasone
    Paramethasone is an orally active long-acting glucocorticoid. Paramethasone directly inhibits testicular aromatase, thereby reducing the synthesis of estradiol. Paramethasone suppresses the basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone also decreases circulating levels of dihydrotestosterone, androstenedione and estradiol in male animals. Paramethasone inhibits cartilage degeneration and alleviates joint pathological damage in osteoarthritis models. Paramethasone can be used in research related to osteoarthritis and endocrinology.
    Paramethasone
  • HY-151963
    PPARγ/GR modulator 1
    		Agonist
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.
    PPARγ/GR modulator 1
Cat. No. Product Name / Synonyms Application Reactivity