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-15710
    Cort108297
    		Antagonist 99.44%
    Cort108297 is a specific glucocorticoid receptor (GR) antagonist. Cort108297 has a high affinity for GRs with a Ki of 0.45 nM.
    Cort108297
  • HY-B0629
    Mometasone
    		99.13%
    Mometasone is an inhaled glucocorticoid. Mometasone can be used in mild asthma with a low sputum eosinophil level. Mometasone has the potential for the research of chronic hand eczema and rhinosinusitis.
    Mometasone
  • HY-B1013
    Flurandrenolide
    		99.82%
    Fludroxycortide is a synthetic topical steroid with anti-inflammatory effects and has potential for use in skin irritation.
    Flurandrenolide
  • HY-103662
    GW-870086
    		Agonist 99.59%
    GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
    GW-870086
  • HY-106673
    Hydrocortisone buteprate
    		98.11%
    Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders. Hydrocortisone buteprate (Hydrocortisone probutate) is available as a 0.1% cream or ointment formulation.
    Hydrocortisone buteprate
  • HY-14234
    Glucocorticoid receptor agonist
    		Agonist 99.06%
    Glucocorticoid receptor agonist is a Glucocorticoid receptor agonist that acts on Glucocorticoid receptor (GR), progesterone receptor (PR) and mineralocorticoid receptor (MR) with the IC50 values of 2.1 , 1200 and 210 nM, respectively. Glucocorticoid receptor agonist has steroid-like anti-inflammatory properties and may be used to improve metabolism and reduce increased levels of body fat and serum insulin.
    Glucocorticoid receptor agonist
  • HY-16718
    Dagrocorat
    		Agonist 99.90%
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.
    Dagrocorat
  • HY-13570C
    Betamethasone disodium phosphate
    		≥98.0%
    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
  • HY-112710
    ORIC-101
    		Antagonist 99.30%
    ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity. ORIC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ORIC-101
  • HY-145351
    BAY 1003803
    		Agonist 99.85%
    BAY 1003803 is a glucocorticoid receptor agonist for the topical research of psoriasis or severe atopic dermatitis.
    BAY 1003803
  • HY-17461S1
    Cortisone-d8
    		Agonist 98.17%
    Cortisone-d8 is the deuterium labeled Cortisone. 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[1][3][4].
    Cortisone-d<sub>8</sub>
  • HY-77839S
    Cortodoxone-d5
    		Agonist 99.90%
    Cortodoxone-d5 is the deuterium labeled Cortodoxone.
    Cortodoxone-d<sub>5</sub>
  • HY-U00089
    Hydrocortisone cypionate
    		Agonist 98.04%
    Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
    Hydrocortisone cypionate
  • HY-132269
    Isoflupredone
    		Ligand 99.44%
    Isoflupredone belongs to the class of corticosteroids and exerts its effect by binding to glucocorticoid and mineralocorticoid receptors of animals, such as horses. Isoflupredone can be used in wide range of conditions, such as infection and inflammatory diseases.
    Isoflupredone
  • HY-A0158
    Diflorasone
    		Agonist 99.86%
    Diflorasone act as a corticosteroid hormone receptor agonist with anti-inflammatory and immunosuppressive properties. Diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. Diflorasone is used for the research of skin diseases such as eczema or psoriasis.
    Diflorasone
  • HY-148435
    Glucocorticoid receptor agonist-2
    		Agonist 99.65%
    Glucocorticoid receptor agonist-2 (compound 21) is an glucocorticoid receptor agonist with an IC50 value of 6.6 nM. Glucocorticoid receptor agonist-2 can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference of ABBV-3373.
    Glucocorticoid receptor agonist-2
  • HY-14648S
    Dexamethasone-d5
    		Agonist 99.86%
    Dexamethasone-d5 is the 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[1][2].
    Dexamethasone-d<sub>5</sub>
  • HY-157294
    GSK866
    		Agonist ≥98.0%
    GSK866 is a selective glucocorticoid receptor agonist, with an IC50 of 4.6 nM.
    GSK866
  • HY-B0328R
    Triamcinolone (Standard)
    		Inhibitor 98.42%
    Triamcinolone (Standard) is the analytical standard of Triamcinolone. This product is intended for research and analytical applications.
    Triamcinolone (Standard)
  • HY-123352
    ZK 216348
    		Agonist 98.59%
    ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.
    ZK 216348
Cat. No. Product Name / Synonyms Application Reactivity