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-107961
    Diflorasone diacetate
    		99.86%
    Diflorasone diacetate is an anti-inflammatory steroid compound used as locally or topically agent. Diflorasone diacetate is being used for skin disorders to control corticosteroid-responsive dermatoses.
    Diflorasone diacetate
  • HY-134116
    Isoflupredone acetate
    		98.55%
    Isoflupredone acetate is a corticosteroids with anti-inflammatory activity. Isoflupredone acetate can be used for research ketosis, musculoskeletal disorders, hypersensitivity, infections, inflammatory diseases in cows, horse, pigs, et al..
    Isoflupredone acetate
  • HY-14864A
    (S)-Mapracorat
    		Inhibitor 99.85%
    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
    (S)-Mapracorat
  • HY-16718A
    Dagrocorat hydrochloride
    		Agonist 99.85%
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride 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 hydrochloride can be used for the research of rheumatoid arthritis.
    Dagrocorat hydrochloride
  • HY-146564A
    HP210
    		Modulator 98.96%
    HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.
    HP210
  • HY-116691
    Hydrocortisone aceponate
    		Agonist 99.43%
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a potent topical glucocorticoid. Hydrocortisone aceponate can be used for various dermatoses research.
    Hydrocortisone aceponate
  • HY-77839S1
    Cortodoxone-d2
    		Agonist 99.00%
    Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone)[1].
    Cortodoxone-d<sub>2</sub>
  • HY-123352A
    (-)-ZK 216348
    		Agonist 98.92%
    (-)-ZK 216348 is the enantiomer of (+)-ZK 216348 (HY-123352). (+)-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
  • HY-B0636S3
    Triamcinolone acetonide-d6
    		Agonist
    Triamcinolone acetonide-d6 is deuterium labeled Triamcinolone acetonide.
    Triamcinolone acetonide-d<sub>6</sub>
  • HY-152121
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
    		Agonist
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody agent conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation.
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
  • HY-B0260S3
    Methylprednisolone-d7
    		Agonist 99.73%
    Methylprednisolone-d7 is 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].
    Methylprednisolone-d<sub>7</sub>
  • HY-13580S
    Budesonide-d8
    		Agonist
    Budesonide-d8 is the deuterium labeled Budesonide. 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[1][2][3].
    Budesonide-d<sub>8</sub>
  • HY-157294A
    (R)-GSK866
    		Agonist ≥98.0%
    (R)-GSK866 is the (R)-enantiomer of GSK866 (HY-157294). GSK866 is a selective agonist for glucocorticoid receptor with an IC50 of 4.6 nM.
    (R)-GSK866
  • HY-13570A
    Betamethasone hydrochloride
    		Agonist
    Betamethasone hydrochloride is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone hydrochloride accelerates fetal lung maturation and induces gene expression and apoptosis.
    Betamethasone hydrochloride
  • HY-160179
    Glucocorticoid receptor agonist-4
    		Agonist 99.80%
    Glucocorticoid receptor agonist-4 (Compound Preparation 5) is a glucocorticoid receptor agonist that can be conjugated to TNF-α antibodies for the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-4
  • HY-160177
    Glucocorticoid receptor agonist-3
    		Agonist 98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
  • HY-B1900R
    Methylprednisolone succinate (Standard)
    		Agonist 99.73%
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate. This product is intended for research and analytical applications. Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
    Methylprednisolone succinate (Standard)
  • HY-N0583S1
    Hydrocortisone-d7
    		Agonist
    Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
    Hydrocortisone-d<sub>7</sub>
  • HY-B0485R
    Fluocinonide (Standard)
    		Agonist 99.16%
    Fluocinonide (Standard) is the analytical standard of Fluocinonide. This product is intended for research and analytical applications.
    Fluocinonide (Standard)
  • HY-151876
    Glucocorticoid receptor modulator 1
    		Modulator 99.79%
    Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
    Glucocorticoid receptor modulator 1
Cat. No. Product Name / Synonyms Application Reactivity