1. Signaling Pathways
  2. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13571A
    Beclometasone dipropionate
    Agonist 99.89%
    Beclometasone dipropionate, the proagent of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate can be used for asthma .
    Beclometasone dipropionate
  • HY-153345
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
    Agonist 99.67%
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br is an Drug-linker conjugates for ADC that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs).
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
  • HY-B0485
    Fluocinonide
    Agonist 99.63%
    Fluocinonide (Vanos) is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders.
    Fluocinonide
  • HY-B1183
    Hydrocortisone acetate
    Agonist 99.07%
    Hydrocortisone acetate (Hydrocortisone 21-acetate) is a corticosteroid used to reduce swelling, itching and pain caused by minor skin irritations or hemorrhoids.
    Hydrocortisone acetate
  • HY-13681
    Methylprednisolone acetate
    Agonist
    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.
    Methylprednisolone acetate
  • HY-B1834
    Megestrol
    Agonist 99.44%
    Megestrol is an orally active glucocorticoid and progesterone receptor agonist. Megestrol can alleviate anorexia, cachexia or unexplained significant weight loss associated with acquired immunodeficiency syndrome (AIDS). Megestrol may cause manifestations similar to those of glucocorticoids and increase the risk of mental disorders.
    Megestrol
  • HY-103548
    GSK9027
    Agonist 98.59%
    GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone.
    GSK9027
  • HY-B0469R
    Medroxyprogesterone acetate (Standard)
    Medroxyprogesterone acetate (Standard) is the analytical standard of Medroxyprogesterone acetate. This product is intended for research and analytical applications. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
    Medroxyprogesterone acetate (Standard)
  • HY-B1900
    Methylprednisolone succinate
    Agonist 99.67%
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.
    Methylprednisolone succinate
  • HY-13571
    Betamethasone dipropionate
    Modulator 99.40%
    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
    Betamethasone dipropionate
  • HY-B1197
    Amcinonide
    Agonist 99.11%
    Amcinonide is an inhibitor of NO release (IC50 = 3.38 nM). Amcinonide inhibits NNC-induced expression of the proinflammatory genes iNOS, TNF-α, and IL-1β in glial cells. Amcinonide reduces the numbers of T6+/Ia+ cells with a concomitant increase in T6+/Ia- cells. Amcinonide induces a selective reduction in expression of Ia antigens. Amcinonide can also be studied in research for eczematous dermatitis.
    Amcinonide
  • HY-15709
    AL 082D06
    Antagonist 98.92%
    AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
    AL 082D06
  • HY-17461S1
    Cortisone-d8
    Agonist 98.17%
    Cortisone-d8 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone-d<sub>8</sub>
  • HY-120012
    Mizacorat
    Modulator 99.34%
    Mizacorat (AZD9567; compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
    Mizacorat
  • HY-13570C
    Betamethasone disodium phosphate
    99.84%
    Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a kind of corticosteroid, which is commonly used in the intralesional research of keloids.
    Betamethasone disodium phosphate
  • HY-111453
    Velsecorat
    Modulator 99.83%
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
    Velsecorat
  • HY-136239
    Beclomethasone 17-propionate
    Agonist 99.52%
    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.
    Beclomethasone 17-propionate
  • HY-123352
    ZK 216348
    Agonist 99.93%
    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-108243
    AZD5423
    Modulator 99.81%
    AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
    AZD5423
  • HY-14930
    Mirodenafil
    Modulator 99.88%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
Cat. No. Product Name / Synonyms Application Reactivity