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-B0645R
    Prednisolone disodium phosphate (Standard)
    		Agonist
    Prednisolone (disodium phosphate) (Standard) is the analytical standard of Prednisolone (disodium phosphate). This product is intended for research and analytical applications.
    Prednisolone disodium phosphate (Standard)
  • HY-15234S
    Fluticasone furoate-d3
    		Activator
    Fluticasone furoate-d3 is deuterium labeled Fluticasone furoate. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
    Fluticasone furoate-d<sub>3</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-B0154S1
    Fluticasone propionate-d5
    		Agonist
    Fluticasone propionate-d5 is deuterium labeled Fluticasone (propionate). Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity.
    Fluticasone propionate-d<sub>5</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 (Standard) is the analytical standard of Flumethasone pivalate. This product is intended for research and analytical applications. Flumethasone pivalate is a glucocorticoid corticosteroid and a corticosteroid ester. Flumetasone pivalate has anti-inflammatory, antipruritic, and vasoconstrictive activities.
    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 (Vanos) is a glucocorticoid steroid with anti-inflammatory activity that acts on skin diseases.
    Fluocinonide-d<sub>6</sub>
  • HY-113537
    Demegestone
    		Agonist
    Demegestone is an agonist of theprogesterone receptor.
    Demegestone
  • 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-117463
    Dexamethasone beloxil
    Dexamethasone beloxil (AL-2512) is a novel corticosteroid with anti-inflammatory and ocular hypertensive effects .
    Dexamethasone beloxil
  • HY-13683S
    Mifepristone-d3
    		Antagonist
    Mifepristone-d3 is the 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-d<sub>3</sub>
  • 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>
  • HY-125360
    Mazipredone free base
    Mazipredone free base, a glucocorticoid derivative, is an anti-inflammatory and anti-allergic agent. Mazipredone free base is sensitive to oxidation, acidic and basic media.
    Mazipredone free base
Cat. No. Product Name / Synonyms Application Reactivity