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Results for "

progesterone receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

7

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13683
    Mifepristone
    Maximum Cited Publications
    71 Publications Verification

    RU486; RU 38486

    		 Endogenous Metabolite Progesterone Receptor Glucocorticoid Receptor NO Synthase Autophagy Endocrinology Cancer
    Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
    Mifepristone
  • HY-111372
    Finerenone
    5+ Cited Publications

    BAY 94-8862

    		 Mineralocorticoid Receptor Cardiovascular Disease Metabolic Disease
    Finerenone (BAY 94-8862) is a third-generation, selective, and orally active nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50 = 18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (> 500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
    Finerenone
  • HY-109171
    Elinzanetant

    NT-814; BAY3427080

    		 Neurokinin Receptor Cardiovascular Disease Neurological Disease
    Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .
    Elinzanetant
  • HY-111372R
    Finerenone (Standard)

    BAY 94-8862 (Standard)

    		 Reference Standards Mineralocorticoid Receptor Cardiovascular Disease
    Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
    Finerenone (Standard)
  • HY-115625
    AG-205

    		Progesterone Receptor Apoptosis Glycosyltransferase Cancer
    AG-205 is a progesterone receptor membrane component 1 (PGRMC1) antagonist and CGT inhibitor, with an IC50 of 50 μM against rat CGT. AG-205 exhibits antimitotic, antimigratory and anti-invasive activities. AG-205 increases the expression of genes encoding cholesterol biosynthesis pathway or steroidogenic enzymes. AG-205 promotes the regulation of cell cycle by apoptosis and reduces the migratory and invasive capacities of ovarian and breast cancer cells. AG-205 can be used in research related to renal cancer and breast cancer .
    AG-205
  • HY-119433
    Asoprisnil

    J867

    		 Progesterone Receptor Endocrinology
    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human .
    Asoprisnil
  • HY-11028
    PF-02413873

    PF-2413873

    		 Progesterone Receptor Endocrinology
    PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo .
    PF-02413873
  • HY-13683R
    Mifepristone (Standard)
    Maximum Cited Publications
    71 Publications Verification

    RU486 (Standard); RU 38486 (Standard)

    		 Reference Standards Progesterone Receptor Glucocorticoid Receptor NO Synthase Autophagy Endocrinology Cancer
    Mifepristone (Standard) is the analytical standard of Mifepristone. This product is intended for research and analytical applications. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
    Mifepristone (Standard)
  • HY-106389
    Onapristone

    ZK 98299

    		 Progesterone Receptor Cancer
    Onapristone is a progesterone receptor antagonist, with Kds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. Onapristone has antitumor activity .
    Onapristone
  • HY-157493
    PR antagonist 1

    		Progesterone Receptor Endocrinology
    PR antagonist 1 (compound 8) is a selective progesterone receptor (PR) antagonist, and can be used for the research of a variety of progesterone-related diseases and disorders such as endometriosis and uterine fibroids .
    PR antagonist 1
  • HY-13683S
    Mifepristone-d3

    RU486-d3; RU 38486-d3

    		 Progesterone Receptor Glucocorticoid Receptor NO Synthase Autophagy Endocrinology Cancer
    Mifepristone-d3 is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
    Mifepristone-d3
  • HY-12073
    WAY-255348

    		Progesterone Receptor Endocrinology Cancer
    W-255348 is an effective non-steroidal progesterone receptor (PR) antagonist that acquires antagonist activity by binding to and subsequently blocking progesterone induced nuclear accumulation, phosphorylation, and PR promoter interactions. WAY-255348 can be used in the research of reproductive disorders or PR-positive breast cancer .
    WAY-255348
  • HY-13683S2
    Mifepristone-d6

    RU486-d6; RU 38486-d6

    		 Glucocorticoid Receptor Autophagy Endogenous Metabolite NO Synthase Progesterone Receptor Isotope-Labeled Compounds Endocrinology Cancer
    Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
    Mifepristone-d6
  • HY-12738
    PF-3882845

    		Mineralocorticoid Receptor Progesterone Receptor Cardiovascular Disease Metabolic Disease
    PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM .
    PF-3882845
  • HY-111372A
    (Rac)-Finerenone

    (Rac)-BAY 94-8862

    		 Mineralocorticoid Receptor Cardiovascular Disease
    (Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .
    (Rac)-Finerenone
  • HY-14250
    PF-998425

    		Androgen Receptor Endocrinology
    PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .
    PF-998425
  • HY-111372S
    Finerenone-d3

    BAY 94-8862-d3

    		 Mineralocorticoid Receptor Others
    Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
    Finerenone-d3
  • HY-111372S1
    Finerenone-d5
    1 Publications Verification

    BAY 94-8862-d5

    		 Isotope-Labeled Compounds Mineralocorticoid Receptor Cardiovascular Disease
    Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
    Finerenone-d5
  • HY-125839
    OP-3633

    		Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
    OP-3633
  • HY-119482
    Cymipristone

    		Progesterone Receptor Others
    Cymipristone (ZXH-951), a progesterone receptor antagonist, is used potentially for termination of intrauterine pregnancy .
    Cymipristone
  • HY-B0251S
    Eplerenone-d3

    Epoxymexrenone-d3

    		 Isotope-Labeled Compounds Mineralocorticoid Receptor Endogenous Metabolite Cardiovascular Disease
    Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch .
    Eplerenone-d3
  • HY-109171R
    Elinzanetant (Standard)

    NT-814 (Standard); BAY3427080 (Standard)

    		 Reference Standards Neurokinin Receptor Cardiovascular Disease Neurological Disease
    Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
    Elinzanetant (Standard)
  • HY-123163
    JNJ-1250132

    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-125627
    CP-394531

    		Glucocorticoid Receptor Androgen Receptor Neurological Disease Metabolic Disease
    CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .
    CP-394531
  • HY-120767
    Linzagolix choline

    KLH-2109 choline; OBE-2109 choline

    		 GnRH Receptor Inflammation/Immunology Cancer
    Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
    Linzagolix choline
  • HY-14465
    PF 02367982

    		Progesterone Receptor Endocrinology
    PF 02367982 is a potent and select progesterone receptor (PR) antagonist with an IC50 value of 47.3 nM. PF 02367982 has oral activity .
    PF 02367982
  • HY-113889
    ZK112993

    		Progesterone Receptor Cancer
    ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice .
    ZK112993
  • HY-167932
    Mifepristone methochloride

    RU486 methochloride; RU 38486 methochloride

    		 Progesterone Receptor Endocrinology
    Mifepristone (RU486) methochloride is a glucocorticoid antagonist that blocks peripheral glucocorticoid and progesterone receptors. Mifepristone methochloride has been shown to have minimal effects on intraocular pressure in treated rabbits. Mifepristone methochloride was developed as a water-soluble formulation to enhance ocular penetration of the drug.
    Mifepristone methochloride
  • HY-109171S
    Elinzanetant-d3

    NT-814-d3; BAY3427080-d3

    		 Isotope-Labeled Compounds Neurokinin Receptor Cardiovascular Disease Neurological Disease
    Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
    Elinzanetant-d3
  • HY-13683S1
    Mifepristone-13C,d3

    RU486-13C,d3; RU 38486-13C,d3

    		 Isotope-Labeled Compounds Progesterone Receptor Glucocorticoid Receptor NO Synthase Autophagy Endocrinology Cancer
    Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay . Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mifepristone-13C,d3
  • HY-16290
    Lonaprisan

    ZK 230211; BAY86 5044

    		 Progesterone Receptor Endocrinology
    Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC50 of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect .
    Lonaprisan
  • HY-117649
    RU-39411

    		Estrogen Receptor/ERR Cancer
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
    RU-39411
  • HY-119080
    CP8754

    		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-111372B
    (R)-Finerenone

    (R)-BAY 94-8862

    		 Drug Isomer Mineralocorticoid Receptor Cardiovascular Disease
    (R)-Finerenone ((R)-BAY 94-8862) is the R-isomer of Finerenone (HY-111372). Finerenone is a third-generation selective, orally active, non-steroidal mineralocorticoid receptor (MR) antagonist (IC50 = 18 nM). Compared with glucocorticoid receptors (GR), androgen receptors (AR), and progesterone receptors (AR), Finerenone shows good selectivity (> 500-fold). Finerenone has potential application prospects in studies of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease .
    (R)-Finerenone

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