Glucocorticoid Receptor

Related Products

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.

Glucocorticoid Receptor Related Products (237)
Antibodies (4)

By Effects:	Inhibitors (15) Agonists (152) Antagonists (20) Activators (8) Modulators (29)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

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].

HY-U00298

Amebucort	Modulator	≥99.0%
Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.

HY-139556

Zavacorilant	Modulator
Zavacorilant is capable of modulating glucocorticoid receptor (GR).

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.

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.

HY-13683S1

Mifepristone-¹³C,d₃	Antagonist
Mifepristone-¹³C,d₃ is the ¹³C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-B0154S1

Fluticasone propionate-d₅	Agonist
Fluticasone propionate-d₅ is deuterium labeled Fluticasone (propionate). Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].

HY-13571AS1

Beclometasone dipropionate-d₁₀	Agonist
Beclometasone dipropionate-d₁₀ is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].

HY-B1121S

Flunisolide-d₆	Activator
Flunisolide-d₆ is the deuterium labeled Flunisolide. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.

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.

HY-113537

Demegestone	Agonist
Demegestone is an agonist of theprogesterone receptor.

HY-17358S

Loteprednol Etabonate-d₅	Agonist
Loteprednol Etabonate-d₅ is a deuterium labeled Loteprednol etabonate. Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology[1][2][3].

HY-13609S1

Deflazacort-d₇	Agonist
Deflazacort-d₇ is the deuterium labeled Deflazacort. Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant[1].

HY-B0636S

Triamcinolone acetonide-d₇	Agonist
Triamcinolone acetonide-d₇ is the deuterium labeled Triamcinolone acetonide. Triamcinolone acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone.

HY-13683S

Mifepristone-d₃	Antagonist
Mifepristone-d₃ is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1].

HY-13571S

Betamethasone dipropionate-d₁₀	Modulator
Betamethasone dipropionate-d₁₀ is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.

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).

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.

HY-B1829

Dexamethasone phosphate	Agonist
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a biologically inactive compound which undergoes dephosphorylation by intra-erythrocyte enzymes. The active metabolite, Dexamethasone, is then released into the circulation by simple passive diffusion through cell membranes. Dexamethasone phosphate disodium-encapsulated erythrocyte has the potential for steroid-dependent ulcerative colitis research.

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Glucocorticoid Receptor

Glucocorticoid Receptor

Glucocorticoid Receptor Related Products (237)

Antibodies (4)

Glucocorticoid Receptor Related Products (237):