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-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-107932
    Triamcinolone diacetate
    Triamcinolone diacetate is a synthetic derivative of glucocorticoid. Triamcinolone diacetate has anti-inflammatory activity. Triamcinolone diacetate can be used in research on dermatomyositis, Bell's palsy and rheumatoid arthritis.
    Triamcinolone diacetate
  • 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-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-134520R
    21-Deacetoxy deflazacort (Standard)
    21-Deacetoxy deflazacort (Standard) is the analytical standard of 21-Deacetoxy deflazacort. This product is intended for research and analytical applications. 21-Deacetoxy deflazacort is a dehydrogenated derivative of Deflazacort (HY-13609), a glucocorticoid, an inactive precursor that is rapidly converted to the active metabolite 21-Desacetyldeflazacort. Deflazacort acts as an anti-inflammatory and immunosuppressant.
    21-Deacetoxy deflazacort (Standard)
  • HY-149165
    Glucocorticoid receptor modulator 2
    		Modulator 99.84%
    Glucocorticoid receptor modulator 2 (Example 1) is a glucocorticoid receptor modulator, with an IC50 value less than 100 nM. Glucocorticoid receptor modulator 2 can be used for research of inflammatory and immune diseases.
    Glucocorticoid receptor modulator 2
  • HY-17461AR
    Cortisone acetate (Standard)
    		Agonist
    Cortisone acetate (Standard) is the analytical standard of Cortisone acetate. This product is intended for research and analytical applications. Cortisone acetate (Cortisone 21-acetate), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acetate acts as an immunosuppressant and anti-inflammatory agent. Cortisone acetate can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone acetate (Standard)
  • HY-171081
    Glucocorticoid receptor agonist-6
    		Agonist
    Glucocorticoid receptor agonist-6 (Compound A) is a Glucocorticoid receptor (GR) agonist. Glucocorticoid receptor agonist-6 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).
    Glucocorticoid receptor agonist-6
  • HY-119296R
    Cloprednol (Standard)
    Cloprednol (Standard) is the analytical standard of Cloprednol. This product is intended for research and analytical applications. Cloprednol is an orally active synthetic glucocorticoid. Cloprednol has anti-inflammatory activity, and can be used in the research of asthma.
    Cloprednol (Standard)
  • HY-19604
    SQ 26490
    SQ 26490 is an active corticoid, moderate-potency edema formation inhibitor. SQ 26490 inhibits edema formation in rats.
    SQ 26490
  • HY-144397
    LEO 134310
    		Agonist
    LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases.
    LEO 134310
  • HY-117965
    Miricorilant
    		Modulator
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders.
    Miricorilant
  • HY-134520
    21-Deacetoxy deflazacort
    21-Deacetoxy deflazacort is a dehydrogenated derivative of Deflazacort (HY-13609), a glucocorticoid, an inactive precursor that is rapidly converted to the active metabolite 21-Desacetyldeflazacort. Deflazacort acts as an anti-inflammatory and immunosuppressant.
    21-Deacetoxy deflazacort
  • HY-B1540S
    Beclomethasone-d5
    		Agonist
    Beclomethasone-d5 is the deuterium labeled Beclometasone. Beclometasone (Beclomethasone) is a prototype glucocorticoid receptor agonist.
    Beclomethasone-d<sub>5</sub>
  • HY-B0214S2
    Prednisone-d4
    		Agonist
    Prednisone-d4 is deuterated labeled Prednisone (HY-B0214). Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.
    Prednisone-d<sub>4</sub>
  • HY-112255
    J9
    		Activator
    J9 is a small molecule that reverses Dexamethasone (HY-14648) resistance in T-cell acute lymphoblastic leukemia. J9 is lethal to CUTLL1 cells only in the presence of Dexamethasone. J9 inhibits CUTLL1 cell growth with an EC50 of 28 μM in combination with Dexamethasone.
    J9
  • HY-160180
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal
    		Agonist
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal (Compound Preparation 9) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-4 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal
  • HY-N12744
    2-O-trans-p-Coumaroylalphitolic acid
    		Modulator
    2-O-trans-p-Coumaroylalphitolic acid (Zj7) is a triterpene which can be extracted from jujube plants. 2-O-trans-P-Coumaroyl alphitolic acid is a selective modulator of glucocorticoid receptor (GR). 2-O-trans-P-coumaroyl alphitolic acid can be used in the study of obesity.
    2-O-trans-p-Coumaroylalphitolic acid
Cat. No. Product Name / Synonyms Application Reactivity