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-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[1][2][3].
    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[1].
    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[1].
    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
  • 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-136239R
    Beclomethasone 17-propionate (Standard)
    		Agonist
    Beclomethasone 17-propionate (Standard) is the analytical standard of Beclomethasone 17-propionate. This product is intended for research and analytical applications. Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3].
    Beclomethasone 17-propionate (Standard)
  • 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[3][4].
    Methylprednisolone-d<sub>2</sub>
Cat. No. Product Name / Synonyms Application Reactivity