Glucocorticoid Receptor
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.
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Glucocorticoid Receptor Inhibitors
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Glucocorticoid Receptor Agonists
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Glucocorticoid Receptor Antagonists
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Glucocorticoid Receptor Modulators
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Glucocorticoid Receptor Substrate
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Glucocorticoid Receptor Ligands
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Glucocorticoid Receptor Related Products (411)
Related Products (411)
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Antibodies (4)
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(D-Asn28)-Exenatide
0 ImagesCat. No.: HY-P4407CAS No.: 2022972-66-1(D-Asn28)-Exenatide is an Exenatide (HY-13443) impurity. Exenatide is a long-acting glucagon-like peptide-1 receptor agonist.
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Glucocorticoid receptor/IL-6-IN-1
0 ImagesCat. No.: HY-176876CAS No.: 1198784-71-2Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 120 nM and 59 nM, respectively). Glucocorticoid receptor/IL-6-IN-1 inhibits IL-6-induced JAK/STAT3 phosphorylation, blocking inflammatory cytokine transcription. Glucocorticoid receptor/IL-6-IN-1 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma.
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Methylprednisolone acetate (Standard)
0 ImagesMethylprednisolone acetate (Standard) is the analytical standard of Methylprednisolone acetate. This product is intended for research and analytical applications. Methylprednisolone acetate, a prednisolone derivative, is a corticosteroid hormone. Methylprednisolone acetate can relieve pain and swelling that occurs with arthritis and other joint disorders in vivo.
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Flocoumafen (Standard)
0 ImagesCat. No.: HY-111186RCAS No.: 90035-08-8Synonyms: WL 108366 (Standard)Flocoumafen (Standard) is the analytical standard of Flocoumafen. This product is intended for research and analytical applications. Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.
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Desoximetasone (Standard)
0 ImagesDesoximetasone (Standard) is the analytical standard of Desoximetasone (HY-17570). This product is intended for research and analytical applications. Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.
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Rimexolone
0 ImagesCat. No.: HY-B1754CAS No.: 49697-38-3Synonyms: Org 6216; RimexelRimexolone (Org 6216) is a glucocorticoid steroid with anti-inflammatory activity. Rimexolone can be used as a 1% ophthalmic suspension for the management of ocular inflammation.
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Glucocorticoid receptor/NF-κB modulator-1
0 ImagesCat. No.: HY-161520Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model.
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Betamethasone dipropionate-d6
0 ImagesCat. No.: HY-13571S2Synonyms: Betamethasone 17,21-dipropionate-d6Betamethasone dipropionate-d6 (Betamethasone 17,21-dipropionate-d6) is the deuterium labeled Betamethasone dipropionate (HY-13571). Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
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Glucocorticoid receptor modulator 3
0 ImagesCat. No.: HY-163672CAS No.: 2688785-13-7Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases.
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Butixocort propionate
0 ImagesCat. No.: HY-19653ACAS No.: 98449-05-9Synonyms: JO 1222Butixocort propionate (JO 1222), a corticosteroid, is a potent Glucocorticoid Receptor agonist. Butixocort propionate exhibits anti-inflammatory activity. Butixocort propionate can be used for the researches of inflammation, immunology and metabolic disease, such as asthma and arthritis.
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AL-438
0 ImagesCat. No.: HY-114154CAS No.: 239066-73-0AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity.
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BI 653048 phosphate
0 ImagesCat. No.: HY-12946ACAS No.: 1198784-97-2BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
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Mal-Val-Cit-PABC-Dexamethasone
0 ImagesCat. No.: HY-186292CAS No.: 1285684-41-4Mal-Val-Cit-PABC-Dexamethasone is a conjugate of the glucocorticoid receptor agonist Dexamethasone (HY-14648) and a ADC linker, which can be used for the synthesis of antibody-drug conjugates (ADC). Mal-Val-Cit-PABC-Dexamethasone is designed to deliver immunosuppressants to monocytes and/or monocyte-derived cells in a targeted manner.
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GSK-3β/G9a-IN-1
0 ImagesCat. No.: HY-W657887CAS No.: 154866-92-9GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.
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Fluocinolone acetonide-13C3
0 ImagesCat. No.: HY-W777281CAS No.: 1262192-25-5Fluocinolone acetonide-13C3 is the 13C-labeled Fluocinolone (Acetonide) (HY-B0415). Fluocinolone is a glucocorticoid glucocorticoid receptor agonist. Fluocinolone is effective in preventing both lipid accumulation and inflammation. Fluocinolone can promote the proliferation of DPCs and has the potential role in repairing injured pulp tissues. Fluocinolone can be used to study the prevention of chemotherapy-induced peripheral neuropathy caused by Paclitaxel (HY-B0015).
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Dexamethasone acetate-d5
0 ImagesCat. No.: HY-W744577Synonyms: Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5Dexamethasone acetate-d5 (Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5) is the deuterium labeled Dexamethasone acetate (HY-14648A). Dexamethasone acetate (Dexamethasone 21-acetate) is the acetate form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone acetate has a longer duration of action than Dexamethasone. Dexamethasone acetate can accumulate at inflammatory sites, in mouse liver and mouse lung via nanostructured lipid carriers. Dexamethasone acetate can be used to prepare topical formulations for studies related to sensorineural hearing loss, γ-carrageenan-induced paw edema, chronic active hepatitis, pulmonary diseases, and inflammation after vitreoretinal surgery.
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Glucocorticoid receptor-IN-2
0 ImagesCat. No.: HY-142942CAS No.: 2664932-65-2Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV.
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Methylprednisolone-d4
0 ImagesCat. No.: HY-B0260S2Synonyms: U 7532-d4Methylprednisolone-d4 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.
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Betamethasone-d5-1
0 ImagesCat. No.: HY-13570S1CAS No.: 2244574-92-1Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.
