21 Results for "

human glucocorticoid receptors

" in MedChemExpress (MCE) Product Catalog:
Products (21)

21 Results for "human glucocorticoid receptors" in MCE Product Catalog:

1
1 Cited Publications
Cat. No.: HY-B1095
CAS No.: 302-22-7
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 .
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1
1 Cited Publications
Cat. No.: HY-113854
CAS No.: 1034148-15-6
Purity:  99.90%
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 .
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Cat. No.: HY-129630
CAS No.: 53-02-1
Purity:  99.91%
Tetrahydrocortisol is a metabolite of Hydrocortisone (HY-N0583) that fails to activate glucocorticoid receptor. Tetrahydrocortisol inhibits Dexamethasone (HY-14648)-induced formation of cross-linked actin networks. Tetrahydrocortisol acts as a synergist to enhance the activity of anticancer agents. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, ocular hypertension, lung cancer and breast cancer .
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Cat. No.: HY-164894
ABBV-3373 is an anti-TNF antibody-drug conjugate (ADC). ABBV-3373 consists of a fully human TNF antibody Adalimumab (HY-P9908) conjugated to a glucocorticoid receptor agonist (HY-148436). ABBV-3373 can be used for the research of rheumatoid arthritis .
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Cat. No.: HY-W010162
CAS No.: 1948-31-8
Synonyms: L-Alanyl-L-alanine; Ala-Ala
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 .
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Cat. No.: HY-16718
CAS No.: 1044535-52-5
Synonyms: PF-00251802
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 .
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Cat. No.: HY-N3741
CAS No.: 18296-45-2
Synonyms: Didrovaltratum
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 .
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Cat. No.: HY-164807
CAS No.: 1489236-55-6
Target:  

HyT Androgen Receptor HSP

Research Areas:  

Cancer

SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the AR F876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer .
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Cat. No.: HY-106827
CAS No.: 74513-62-5
Synonyms: RU 27987
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 .
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Cat. No.: HY-160180
CAS No.: 3014393-37-1
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 .
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Cat. No.: HY-123163
CAS No.: 240805-96-3
Synonyms: RWJ-66826; RTI-6617-003
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) .
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Cat. No.: HY-16718A
CAS No.: 1044535-61-6
Synonyms: PF-00251802 hydrochloride
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 .
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Cat. No.: HY-N9921
CAS No.: 163597-24-8
Antcin A is an orally active modulator of p53 and glucocorticoid receptor (GR), with an IC50 of 8.55 μM against human GR. Through transcriptional activation of p53, Antcin A induces miR-200c and inhibits ZEB1, regulates epithelial-mesenchymal transition markers, and suppresses cancer cell migration/invasion. Antcin A activates GR, inhibits Na +/K +-ATPase and NLRP3 inflammasome assembly, pyroptosis (pyroptosis) and pro-inflammatory cytokine release, reduces hepatic lipid deposition, improves liver function, and reverses metabolic changes induced by the SARS-CoV-2 spike protein. Antcin A can be used in research related to breast cancer, head and neck cancer, non-alcoholic fatty liver disease, and coronavirus disease 2019 (COVID-19) .
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Cat. No.: HY-160178
CAS No.: 3014393-35-9
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 .
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Cat. No.: HY-131543
CAS No.: 105012-15-5
Synonyms: RU 42698
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% .
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Cat. No.: HY-131543S
Synonyms: RU 42698-d6
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% .
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Cat. No.: HY-119080
CAS No.: 532435-68-0
Target:  

Progesterone Receptor

Research Areas:  

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 .
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Cat. No.: HY-182965
CAS No.: 2756355-59-4
Glucocorticoid receptor antagonist-1 is an orally active glucocorticoid receptor (GR) antagonist with an IC50 of 27 nM and a Ki value of 32 nM, and it exhibits low agonist activity. Glucocorticoid receptor antagonist-1 shows moderate inhibitory effects on CYP2C9 and CYP2D6, and potent inhibitory effect on CYP2C8. Glucocorticoid receptor antagonist-1 prevents Olanzapine (HY-14541)-induced weight gain in female rats. Glucocorticoid receptor antagonist-1 can be used in studies related to weight gain .
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Cat. No.: HY-P992450

Target:  

TNF Receptor

Research Areas:  

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 .
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Cat. No.: HY-179476
CAS No.: 847232-54-6
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 .
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