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human glucocorticoid receptor

" in MedChemExpress (MCE) Product Catalog:

16

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129630

    Microtubule/Tubulin Neurological Disease Cancer
    Tetrahydrocortisol is a cortisol metabolite that inhibits dexamethasone-induced formation of cross-linked actin networks. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, glucocorticoid-induced ocular hypertension, Lewis lung carcinoma, and EMT-6 mouse breast cancer .
    Tetrahydrocortisol
  • HY-B1095
    Chlormadinone acetate
    1 Publications Verification

    Progesterone Receptor Androgen Receptor Glucocorticoid Receptor GABA Receptor Neurological Disease Metabolic Disease
    Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .
    Chlormadinone acetate
  • HY-W010162

    L-Alanyl-L-alanine; Ala-Ala

    Amino Acid Derivatives Others
    H-Ala-Ala-OH is a substrate of human intestinal oligopeptide transporter (PEPT1/SLC15A1), with an IC50 of 0.25 mM and an EC50 of 0.08 mM against human PEPT1. When used as a dipeptide linker in antibody-drug conjugates (ADCs) loaded with glucocorticoid receptor regulator payloads, H-Ala-Ala-OH enables efficient intracellular payload release .
    H-Ala-Ala-OH
  • HY-113854
    AZD2906
    1 Publications Verification

    Glucocorticoid Receptor Cardiovascular Disease Endocrinology
    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
    AZD2906
  • HY-16718

    PF-00251802

    Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
    Dagrocorat
  • HY-N3741

    Didrovaltratum

    Calcium Channel Reactive Oxygen Species (ROS) Autophagy Inflammation/Immunology Cancer
    Didrovaltrate (Didrovaltratum) is an L-type calcium channel blocker, ROS scavenger, autophagy enhancer, and lipid accumulation inhibitor. Didrovaltrate blocks L-type calcium currents in a concentration-dependent manner, shifts the current-voltage curve upward, modulates steady-state inactivation kinetics, and inhibits the nuclear translocation of glucocorticoid receptors. Didrovaltrate reduces ROS levels, downregulates the expression of muscle atrophy-related genes, enhances autophagy via lipophagy, and decreases Oleic acid-induced lipid accumulation. Didrovaltrate exhibits cytotoxic activity against cancer cells. Didrovaltrate can be used in research related to skeletal muscle atrophy, non-alcoholic fatty liver disease, breast cancer, lung cancer, gastric cancer, and prostate cancer .
    Didrovaltrate
  • HY-106827

    RU 27987

    Progesterone Receptor Androgen Receptor Phosphatase Metabolic Disease
    Trimegestone (RU 27987) is an orally active, selective progestogen and PR ligand, with an IC50 of 7.6 nM for hPR, 4.4 nM for rabbit PR, and 3.3 nM for rat PR. Trimegestone induces Alkaline phosphatase activity. Trimegestone exhibits antiandrogenic activity (IC50 = 303 nM). Trimegestone can be used in research related to menopausal symptoms and osteoporosis .
    Trimegestone
  • HY-160180

    TNF Receptor Glucocorticoid Receptor Drug-Linker Conjugates for ADC Inflammation/Immunology
    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-123163

    RWJ-66826; RTI-6617-003

    Progesterone Receptor Glucocorticoid Receptor Androgen Receptor Estrogen Receptor/ERR Endocrinology Cancer
    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-16718A

    PF-00251802 hydrochloride

    Glucocorticoid Receptor Cytochrome P450 Inflammation/Immunology Endocrinology
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
    Dagrocorat hydrochloride
  • HY-160178

    TNF Receptor Glucocorticoid Receptor Drug-Linker Conjugates for ADC Inflammation/Immunology
    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 .
    Glucocorticoid receptor agonist-3 Ala-Ala-Mal
  • HY-131543

    RU 42698

    Endogenous Metabolite Glucocorticoid Receptor Metabolic Disease
    22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcoholic metabolite with antiprogestational and antiglucocorticoidal activities, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. The relative binding affinity of 22-Hydroxy Mifepristone to the human glucocorticoid receptor is 48% .
    22-Hydroxy mifepristone
  • HY-131543S

    RU 42698-d6

    Isotope-Labeled Compounds Others
    22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone (HY-131543). 22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcoholic metabolite with antiprogestational and antiglucocorticoidal activities, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. The relative binding affinity of 22-Hydroxy Mifepristone to the human glucocorticoid receptor is 48% .
    22-Hydroxy Mifepristone-d6
  • HY-119080

    Progesterone Receptor Endocrinology Cancer
    CP8754 is an orally active, selective human progesterone receptor (hPR) antagonist that blocks progesterone-mediated signaling pathways. CP8754 competitively inhibits the binding of [ 3H]-progesterone to hPR. And in vitro, CP8754 inhibits progesterone-dependent exogenous luciferase and endogenous alkaline phosphatase expression; while in vivo, CP8754 inhibits rabbit endometrial transformation. CP8754 does not significantly bind to human glucocorticoid receptors (hGR), estrogen receptors (hER), or rat androgen receptors (rAR). CP8754 can be used in the study of progesterone-related diseases such as breast cancer, endometriosis, uterine fibroids, and meningioma, as well as hormone-dependent tumors .
    CP8754
  • HY-P992450

    TNF Receptor Cancer
    REGN6569 is a fully human IgG1 monoclonal antibody targeting glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) with high specificity for GITR. REGN6569 exerts stronger in vitro antibody-dependent cell-mediated cytotoxicity (ADCC) against regulatory T cells expressing GITR. REGN6569 selectively depletes regulatory T cells via antibody-dependent cell-mediated cytotoxicity and increases the proportion of proliferative natural killer (NK) cells in peripheral blood. REGN6569 is applicable for advanced solid malignancies. Isotype control: HY-P99001 .
    REGN6569
  • HY-179476

    Androgen Receptor Endogenous Metabolite Inflammation/Immunology Cancer
    3-Oxochol-5-en-24-oic acid is a rare bile acid produced by the intestinal microbiota. 3-Oxochol-5-en-24-oic acid is a potent antagonist of the human androgen receptor (hAR), with an IC50 of 119.4 nM. 3-Oxochol-5-en-24-oic acid has no significant agonistic or antagonistic effects on estrogen receptors (ER) or glucocorticoid receptors (GR). 3-Oxochol-5-en-24-oic acid effectively inhibits the growth of prostate cancer cells. In animal models, it enhances the efficacy of anti-PD-1 therapy by regulating the differentiation of CD8 + T cells. 3-Oxochol-5-en-24-oic acid can be used for research on regulating host immunity and anti-tumor studies .
    3-Oxochol-5-en-24-oic acid

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