1. Signaling Pathways
  2. GPCR/G Protein
  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.

Glucocorticoid Receptor 相关产品 (69):

Cat. No. Product Name Effect Purity
  • HY-14648
    Dexamethasone Agonist 99.86%
    Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体 (glucocorticoid receptor) 激动剂。Dexamethasone 还显着降低中性粒细胞的 CD11b,CD18 和 CD62L 表达,以及单核细胞的 CD11b 和 CD18L 表达。
  • HY-N0583
    Hydrocortisone Agonist 99.90%
  • HY-13683
    Mifepristone Antagonist 98.67%
    Mifepristone是黄体酮受体 (PR) 和糖皮质激素受体 (GR) 拮抗剂,体外实验中的 IC50 值分别为0.2 nM 和2.6 nM。
  • HY-B1618
    Corticosterone Agonist 99.70%
  • HY-B0469
    Medroxyprogesterone acetate 99.82%
    Medroxyprogesterone acetate 是一种广泛使用的合成类固醇,与孕酮 (progesterone),雄激素 (androgen) 和糖皮质激素受体 (glucocorticoid receptors) 都有作用。
  • HY-109017
    Vamorolone Agonist
    Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。
  • HY-12946
    BI 653048 Inhibitor
    BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂,其 IC50 值为 55 nM。BI 653048 抑制 CP1A2,CYP2D6,CYP2C9,CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103),它也是一种 HCV NS3 protease 抑制剂,可以减少感染丙型肝炎病毒的病毒载量。
  • HY-B0727
    Betamethasone valerate Agonist
    Betamethasone valerate (Betamethasone 17-valerate) 是 Betamethasone 的 17 戊酸酯,是一种具有抗炎活性的局部皮质类固醇,有抗炎活性。Betamethasone valerate 可用于治疗复发性口疮。Betamethasone valerate 抑制放射标记的糖皮质激素地塞米松 (3H dexamethasone) 与人表皮和小鼠皮肤的结合,IC50 分别为 5 和 6 nM。
  • HY-B1829A
    Dexamethasone phosphate disodium Agonist 99.68%
    Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.
  • HY-17463
    Prednisolone Agonist 99.92%
  • HY-B0260
    Methylprednisolone Agonist 99.67%
  • HY-B0214
    Prednisone Agonist 99.35%
    Prednisone (Adasone)是皮质类固醇试剂,有免疫抑制作用。
  • HY-17461
    Cortisone Agonist 99.90%
  • HY-B0328
    Triamcinolone Inhibitor 99.15%
  • HY-B0154
    Fluticasone (propionate) Agonist 99.97%
  • HY-N0835
    (20S)-Protopanaxatriol Agonist >98.0%
    (20S)-Protopanaxatriol 是人参皂苷的代谢物,通过 glucocorticoid receptoroestrogen receptor 起作用,同时为 LXRα 的抑制剂。
  • HY-B0625
    Ciclesonide Agonist 98.95%
  • HY-14648A
    Dexamethasone acetate Agonist
    Dexamethasone (Dexamethasone 21-acetate) 是糖皮质素类甾体化合物,有抗炎和免疫抑制活性。
  • HY-13580
    Budesonide Agonist >98.0%
  • HY-14864
    Mapracorat Agonist 99.40%
    Mapracorat 是新型的非甾类有选择性的 glucocorticoid receptor 激动剂。
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