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-160177
    Glucocorticoid receptor agonist-3
    		Agonist 98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
  • 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
  • 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-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
  • HY-125096
    C108297
    		Modulator 99.97%
    C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation.
    C108297
  • HY-136340
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
    		Agonist 99.93%
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione is an intermediate of delta 9,11 steroids synthesis, for example, Vamorolone (HY-109017). The delta 9,11 steroids are modifications of glucocorticoids and has anti-inflammatory properties. The delta 9,11 steroids are agents for protection against cell damage (lipid peroxidation) and inhibition of neovascularization.
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
  • HY-160178
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
    		Agonist 99.72%
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal (Compound Preparation 8) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-3 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
  • HY-164860
    Glucocorticoid receptor agonist-5
    		Agonist 99.95%
    Glucocorticoid receptor agonist-5 (compound 4), a glucocorticoid molecule, is a potent glucocorticoid receptor agonist. Glucocorticoid receptor agonist-5 shows anti-inflammatory and immunosuppressive activity. Glucocorticoid receptor agonist-5 is used as an ADC Cytotoxin for antibody-drug conjugate.
    Glucocorticoid receptor agonist-5
  • HY-U00298
    Amebucort
    		Modulator ≥99.0%
    Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
    Amebucort
  • HY-139556
    Zavacorilant
    		Modulator
    Zavacorilant is capable of modulating glucocorticoid receptor (GR).
    Zavacorilant
  • HY-B0603
    Fluticasone
    		Agonist
    Fluticasone is an inhaled corticosteroid used for respiratory research. Fluticasone is a Smo agonist with an IC50 value of 99 nM. Fluticasone activates Hedgehog signaling and promotes the proliferation of primary neuronal stem or precursor cells.
    Fluticasone
  • 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-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-113537
    Demegestone
    		Agonist
    Demegestone is an agonist of theprogesterone receptor.
    Demegestone
  • HY-117463
    Dexamethasone beloxil
    Dexamethasone beloxil (AL-2512) is a novel corticosteroid with anti-inflammatory and ocular hypertensive effects .
    Dexamethasone beloxil
  • HY-159695A
    IONIS-GCCRRx sodium
    		Antagonist
    IONIS-GCCRRx (ISIS 426115) sodium, a glucocorticoid receptor antagonist, is a 2'-O-methoxyethyl (2'-MOE) antisense oligonucleotide (ASO).
    IONIS-GCCRRx sodium
  • 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
Cat. No. Product Name / Synonyms Application Reactivity