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-B1203S
    Fludrocortisone-d5
    		Agonist
    Fludrocortisone-d5 (9α-Fludrocortisone-d5) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
    Fludrocortisone-d<sub>5</sub>
  • HY-13571S1
    Betamethasone dipropionate-d5
    		Modulator
    Betamethasone dipropionate-d5 (Betamethasone 17,21-dipropionate-d5) is deuterium-labeled Betamethasone dipropionate (HY-13571).
    Betamethasone dipropionate-d<sub>5</sub>
  • HY-14648S2
    Dexamethasone-d4
    		Agonist 98.93%
    Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
    Dexamethasone-d<sub>4</sub>
  • HY-139556
    Zavacorilant
    		Modulator
    Zavacorilant is capable of modulating glucocorticoid receptor (GR).
    Zavacorilant
  • HY-125839
    OP-3633
    		Antagonist
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism.
    OP-3633
  • HY-13683S1
    Mifepristone-13C,d3
    		Antagonist
    Mifepristone-13C,d3 is the 13C- and deuterium labeled Mifepristone. 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-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mifepristone-<sup>13</sup>C,d<sub>3</sub>
  • HY-13571AS1
    Beclometasone dipropionate-d10
    		Agonist
    Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release.
    Beclometasone dipropionate-d<sub>10</sub>
  • HY-107949R
    Flumethasone pivalate (Standard)
    		Ligand
    Flumethasone pivalate (Flumethasone 21-pivalate) (Standard) is the analytical standard of Flumethasone pivalate (HY-107949). This product is intended for research and analytical applications. Flumethasone pivalate is a glucocorticoid and a topical corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive actions. Flumethasone pivalate inhibits foreign body granuloma formation. Flumethasone pivalate can be used for the researches of dermatitis, eczema, and psoriasis.
    Flumethasone pivalate (Standard)
  • HY-B0878S
    Halobetasol propionate-d5
    Halobetasol propionate-d5 (BMY-30056-d5) is deuterium labeled Halobetasol propionate (HY-B0878). Halobetasol propionate (BMY-30056) is a synthetic glucocorticoid corticosteroid. Halobetasol propionate exhibits anti-inflammatory, antipruritic, and vasoconstrictive properties. Halobetasol propionate can be used for the study of psoriasis.
    Halobetasol propionate-d<sub>5</sub>
  • HY-B1121S
    Flunisolide-d6
    		Activator
    Flunisolide-d6 is the deuterium labeled Flunisolide. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
    Flunisolide-d<sub>6</sub>
  • HY-146561
    S-HP210
    		Modulator 98.12%
    S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.
    S-HP210
  • HY-B0485S
    Fluocinonide-d6
    		Agonist
    Fluocinonide-d6 is deuterated labeled Fluocinonide (HY-B0485). Fluocinonide is a glucocorticoid with anti-inflammatory and vasoconstrictor properties. Fluocinonide can be used for the research of oral vesiculoerosive diseases and inflammatory dermatoses.
    Fluocinonide-d<sub>6</sub>
  • HY-113537
    Demegestone
    		Agonist
    Demegestone is an agonist of theprogesterone receptor.
    Demegestone
  • HY-125627
    CP-394531
    		Antagonist
    CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease.
    CP-394531
  • HY-17358S
    Loteprednol Etabonate-d5
    		Agonist
    Loteprednol Etabonate-d5 is a deuterium labeled Loteprednol etabonate. Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology.
    Loteprednol Etabonate-d<sub>5</sub>
  • HY-13609S1
    Deflazacort-d7
    		Agonist
    Deflazacort-d7 is the deuterium labeled Deflazacort. Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant.
    Deflazacort-d<sub>7</sub>
  • HY-B0636S
    Triamcinolone acetonide-d7
    		Agonist
    Triamcinolone acetonide-d7 is the deuterium labeled Triamcinolone acetonide. Triamcinolone acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone.
    Triamcinolone acetonide-d<sub>7</sub>
  • HY-106983
    GR 250495X
    		Agonist
    GR 250495X is an inhaled glucocorticoid receptor agonist. GR 250495X is designed as a antedrug, which takes effect locally in the lungs but is rapidly metabolized and inactivated in the bloodstream after entering the systemic circulation, thereby minimizing systemic side effects. GR 250495X can be used in asthma research.
    GR 250495X
  • HY-117463
    Dexamethasone beloxil
    Dexamethasone beloxil (AL-2512) is a novel corticosteroid with anti-inflammatory and ocular hypertensive effects .
    Dexamethasone beloxil
  • HY-13571S
    Betamethasone dipropionate-d10
    		Modulator
    Betamethasone dipropionate-d10 is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate-d<sub>10</sub>
Cat. No. Product Name / Synonyms Application Reactivity