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-B0469R
    Medroxyprogesterone acetate (Standard)
    Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate (Standard)
  • HY-14930
    Mirodenafil
    		Modulator 99.88%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
  • HY-B1051
    Flumethasone
    		Agonist 99.84%
    Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation.
    Flumethasone
  • HY-147293
    Nenocorilant
    		Inhibitor 99.72%
    Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research.
    Nenocorilant
  • HY-B1618S1
    Corticosterone-d4
    		Agonist 99.17%
    Corticosterone-d4 is the deuterium labeled Corticosterone. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
    Corticosterone-d<sub>4</sub>
  • HY-B1183
    Hydrocortisone acetate
    		Agonist 99.14%
    Hydrocortisone acetate (Hydrocortisone 21-acetate) is a corticosteroid used to reduce swelling, itching and pain caused by minor skin irritations or hemorrhoids.
    Hydrocortisone acetate
  • HY-B0878
    Halobetasol propionate
    		99.74%
    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
  • HY-15710
    Cort108297
    		Antagonist 99.80%
    Cort108297 is a specific glucocorticoid receptor (GR) antagonist. Cort108297 has a high affinity for GRs with a Ki of 0.45 nM.
    Cort108297
  • HY-B1214
    Prednisolone acetate
    		Agonist 99.83%
    Prednisolone acetate (Prednisolone 21-acetate) is an adrenocortical hormone active molecule with various pharmacological effects such as anti-inflammatory, anti-allergic, and immune suppression.
    Prednisolone acetate
  • HY-137882
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
    		Agonist 99.94%
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC.
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
  • HY-16722
    Fosdagrocorat
    		Agonist 98.70%
    Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
    Fosdagrocorat
  • HY-111453
    Velsecorat
    		Modulator 99.83%
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
    Velsecorat
  • HY-136239
    Beclomethasone 17-propionate
    		Agonist 99.76%
    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.
    Beclomethasone 17-propionate
  • HY-B0485
    Fluocinonide
    		Agonist 99.63%
    Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.
    Fluocinonide
  • HY-B0248
    Desonide
    		Inhibitor 99.64%
    Desonide is a non-fluorinated corticosteroid anti-inflammatory agent that acts on the glucocorticoid receptor. Desonide can also specifically bind to the mutant huntingtin protein (mHTT), reducing the level and toxicity of mHTT. Desonide can be used in the research of Huntington's disease and inflammatory diseases such as atopic dermatitis.
    Desonide
  • HY-14864
    Mapracorat
    		Agonist 99.40%
    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
    Mapracorat
  • HY-132811
    Dazucorilant
    		Modulator 98.91%
    Dazucorilant (CORT113176) is a selective and high affinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value ＜1 nM in vitro. Dazucorilant can be used for the research of neurological disorders.
    Dazucorilant
  • HY-150701
    INCB13739
    		Inhibitor 99.79%
    INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.
    INCB13739
  • HY-13580R
    Budesonide (Standard)
    		Agonist
    Budesonide (Standard) is the analytical standard of Budesonide. This product is intended for research and analytical applications. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
    Budesonide (Standard)
  • HY-N0583S2
    Hydrocortisone-d4
    		Agonist 99.0%
    Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
    Hydrocortisone-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity