Progesterone Receptors

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  1. Drospirenone is a synthetic hormone used in birth control pills.
  2. Megestrol Acetate is a progesterone derivative with antineoplastic properties
  3. Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
  4. progesterone receptor agonist

    Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
  5. progesterone receptor antagonist

    Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.
  6. progesterone receptor agonist

    Nestoron is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor.
  7. Progesterone receptor agonist

    Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.
  8. Steroid Hormone

    17-Hydroxyprogesterone is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
  9. Progesterone/ERR Agonist

    Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.
  10. progesterone receptor ligand

    Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17?α-hydroxyprogesterone formed from caproic acid.
  11. Progesterone Receptor Agonist

    Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.
  12. progesterone receptor agonist

    Medroxyprogesterone is used in the treatment of renal carcinoma. It is a synthetic progestational hormone used in veterinary practice as an estrus regulator.
  13. Norethindrone acetate is used in combination with estrogen as a contraceptive (oral). It is reasonably anticipated to be a human carcinogen.
  14. Progesterone receptor modulator

    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  15. full progesterone receptor agonist

    Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
  16. progesterone receptor modulator

    Ulipristal (acetate) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
  17. progesterone receptor agonist

    Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
  18. D prostanoid receptor 2 antagonist

    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist.
  19. EGFR Inhibitor, Estrogen Receptor Inhibitor, Progesterone Receptor Inhibitor

    4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions.
  20. Progesterone Receptor Modulator

    Telapristone acetate is a potent progesterone receptor modulator that effectively inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. This compound has demonstrated efficacy in reducing the incidence and progression of both spontaneous and chemically induced mammary tumors in animal models. Telapristone acetate is valuable for research focused on breast and ovarian cancer, providing insights into its therapeutic potential and mechanisms of action.
  21. Progesterone Receptor Antagonist

    Trimegestone acts as a progesterone receptor antagonist, exhibiting a high binding affinity with an IC50 value of 3.3 nM for the rat progesterone receptor. This 19-norpregnane progestin enhances alkaline phosphatase activity, with an EC50 of 0.1 nM, while displaying minimal effects on luciferase activity. Additionally, Trimegestone possesses weak antiandrogenic properties due to its low affinity for the androgen receptor. This compound is valuable in research focusing on contraception and menopausal syndrome investigations.
  22. Progesterone Receptor Agonist

    Demegestone is a selective agonist of the progesterone receptor. It exhibits significant biological activity in modulating progesterone signaling pathways, making it a valuable tool for research in reproductive biology and endocrine function. Its use is relevant for studies involving hormonal regulation, pregnancy, and associated disorders.
  23. Progesterone Receptor Activator

    Cridanimod is a potent activator of the progesterone receptor (PR) that functions primarily through the induction of interferon-alpha (IFNα) and interferon-beta (IFNβ) expression. As a small-molecule immunomodulator and interferon inducer, it plays a crucial role in modulating immune responses. Cridanimod is primarily utilized in research applications focusing on reproductive biology, immunology, and the therapeutic potential of interferon-mediated pathways.
  24. Glucocorticoid/Progesterone Receptor Agoinst

    Megestrol is an orally active glucocorticoid and progesterone receptor agonist. It is primarily utilized to stimulate appetite and promote weight gain in patients experiencing anorexia or cachexia, particularly in those with acquired immunodeficiency syndrome (AIDS). Additionally, megestrol may produce effects similar to glucocorticoids and has the potential to elevate the risk of certain mental health disorders.
  25. Gonadal Steroid Agonist

    Tibolone is a gonadal steroid agonist that exhibits progestagenic, androgenic, and estrogenic properties. It is primarily utilized in research related to postmenopausal osteoporosis, facilitating studies on its effects on bone health and hormonal balance. This compound serves as a valuable tool for investigating the multifaceted roles of steroids in reproductive health and aging.
  26. Synthetic Sexualsteroid

    Allylestrenol is an orally active synthetic sexual steroid with anti-androgenic properties. It has demonstrated the ability to prevent miscarriage in vivo and significantly influences testosterone and progesterone levels in rat models. Additionally, Allylestrenol has been shown to reduce ventral prostate weight in animal studies, making it a valuable reagent for research on reproductive health and endocrine function.
  27. Progesterone Receptor Modulator

    EC 313 is a selective progesterone receptor modulator that effectively targets the progesterone receptor. It demonstrates dose-dependent efficacy in reducing the weight of uterine fibroids and can decrease the expression of estrogen receptor (ER) and progesterone receptor (PR). EC 313 is a valuable tool for investigating the biological mechanisms underlying uterine fibroids and their treatment.
  28. PXR Antagonist

    SJPYT-310 is a selective ligand for the Pregnane X Receptor (PXR), functioning as an antagonist. This compound effectively inhibits PXR-mediated transcriptional activity, providing insights into drug metabolism and cellular responses to xenobiotics. SJPYT-310 is suitable for research applications exploring the role of PXR in pharmacology and toxicology, while demonstrating a favorable safety profile with no significant cytotoxicity observed.
  29. PXR Agonist

    SJB7 is a potent agonist of the pregnane X receptor (PXR), a key regulator in drug metabolism and excretion. By stabilizing the activation function 2 (AF-2) helix in an "inward" conformation, SJB7 enhances PXR-mediated transcriptional activity. This compound is valuable for research applications involving the study of xenobiotic response and the modulation of metabolic pathways.
  30. PXR Ligand

    4-Chloro-2-(trifluoroacetyl)aniline is a potent ligand for the Pregnane X receptor (PXR). This compound is notable for its ability to induce Cyp3a11 mRNA expression, making it a valuable tool in studies of PXR-mediated drug metabolism and detoxification pathways. Its research applications are particularly relevant in pharmacology and toxicology, where understanding PXR activation can inform drug interactions and therapeutic efficacy.
  31. Cholic Acid Conjugated With L-glutamic Acid

    N-Cholyl-L-glutamic acid (GluCA) is a conjugate of cholic acid and L-glutamic acid, primarily targeting the pregnane X receptor (PXR). This compound is known to enhance the expression of PXR and induce the downstream target gene Cyp3a11. N-Cholyl-L-glutamic acid serves as a valuable tool in researching the mechanisms underlying Crohn's disease and other conditions related to altered PXR signaling.
  32. PXR Agonist

    N-Cholyl-L-threonine is a potent agonist of the pregnane X receptor (PXR). This compound, a conjugate of cholic acid and L-threonine, facilitates the modulation of PXR signaling pathways. Its biological activity makes N-Cholyl-L-threonine a valuable reagent for studies related to Crohn's disease and other gastrointestinal disorders.
  33. PXR Activator

    Cholic acid-Glu is a derivative of cholic acid that functions as a PXR (Pregnane X Receptor) activator. It has been shown to increase PXR activation, leading to a significant upregulation of the downstream target gene Cyp3a11 in small intestinal organoid tissue. This compound is particularly relevant for research on inflammatory bowel diseases, such as Crohn’s disease, due to its altered levels in affected individuals.
  34. Progesterone Receptor Agonist

    Clogestone acetate is a potent progesterone receptor agonist that demonstrates notable biological activity in modulating reproductive hormones. In preclinical studies, it has been shown to reduce adrenal and ovarian weights, along with serum and adrenocortical ketone levels in rodent models. This compound is utilized in research exploring the roles of progesterone in various physiological processes and may provide insights into hormonal regulation and endocrine function.
  35. Progesterone Receptor Antagonist

    PF-02413873 is a selective, fully competitive, and orally active nonsteroidal antagonist of the progesterone receptor (PR) with a Ki value of 2.6 nM. This compound effectively inhibits progesterone binding and PR nuclear translocation, demonstrating significant activity in blocking endometrial growth in vivo. PF-02413873 is valuable for research applications focused on reproductive biology and related therapeutic strategies.
  36. Progesterone Receptor Agonist

    Promegestone is a potent progesterone receptor (PR) agonist, recognized for its ability to modulate endocrine pathways. This progestin compound serves as a valuable tool in cancer research, enabling investigations into the hormonal regulation of tumor growth and differentiation. Its selective activity on the PR makes it an important reagent for studies focused on reproductive biology and related therapeutic applications.
  37. Progesterone Receptor

    Norgestimate is a synthetic progestin with selective activity for the progesterone receptor, demonstrating minimal androgenic effects. It is primarily utilized as an oral contraceptive due to its effective progestational properties. In addition to its hormonal applications, Norgestimate serves as a click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, making it valuable for biochemical research and drug development.
  38. Parenteral Progestogen

    Norethisterone enanthate is a long-acting parenteral progestogen that primarily targets progesterone receptors. This compound exhibits significant biological activity in hormone regulation and is utilized in various clinical and research applications, including contraception and hormone replacement therapy. Additionally, norethisterone enanthate features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it valuable as a reagent in click chemistry for diverse biochemical studies.
  39. Contraceptive Agent

    Melengestrol acetate is a synthetic progestin that primarily targets progesterone receptors. It exerts contraceptive effects by promoting endometrial proliferation and maintaining pregnancy, while also delaying menstrual activity. In addition to its use as a contraceptive agent in livestock to suppress estrus and promote growth, melengestrol acetate has demonstrated efficacy in inhibiting both androgen-dependent and independent prostatic tumors in vivo, making it a valuable compound for cancer research applications.
  40. PGRMC1 Antagonist

    AG-205 is a selective antagonist of progesterone receptor membrane component 1 (PGRMC1), exhibiting a potent inhibitory effect on ceramide glucosyltransferase (CGT) with an IC50 of 50 μM in rat models. This compound demonstrates significant antimitotic, antimigratory, and anti-invasive properties, particularly in ovarian and breast cancer cells. AG-205 enhances the expression of genes involved in cholesterol biosynthesis and steroidogenesis while promoting apoptotic regulation of the cell cycle. Its diverse biological activity positions AG-205 as a valuable tool for investigating mechanisms underlying renal and breast cancer progression.
  41. SPRM

    Vilaprisan is a selective progesterone receptor modulator (SPRM) that targets progesterone receptors. It demonstrates notable anti-proliferative effects by inhibiting cell proliferation and promoting apoptosis, particularly in uterine leiomyoma. This compound offers oral efficacy and contributes significantly to research on therapeutic interventions for uterine conditions.
  42. PR Antagonist

    PR Antagonist 1 is a selective progesterone receptor (PR) antagonist that effectively inhibits the activity of PR. This compound is instrumental in studying progesterone-related pathologies, including endometriosis and uterine fibroids, making it valuable for research focused on reproductive health and hormonal regulation. Its specificity for PR allows for targeted investigations into the underlying mechanisms of these disorders.
  43. Progestational Agent

    17α-Hydroxyprogesterone acetate is a progestational agent that primarily acts on progesterone receptors. It exhibits significant progestational activity, contributing to the maintenance of pregnancy. Additionally, this compound has been shown to possess anti-inflammatory effects at the murine maternal-fetal interface, making it relevant for research in reproductive biology and inflammation modulation.
  44. Progesterone Receptor Antagonist

    WAY-255348 is a non-steroidal antagonist of the progesterone receptor (PR), exerting its effects by binding to the PR and inhibiting progesterone-induced nuclear translocation, phosphorylation, and promoter interactions. This compound is useful in the study of reproductive disorders and PR-positive breast cancer, providing valuable insights into PR-mediated signaling pathways and potential therapeutic interventions in these conditions.
  45. Progesterone Receptor Inhibitor

    Mifepristone methochloride is a selective progesterone receptor inhibitor. It functions as a glucocorticoid antagonist, effectively blocking peripheral glucocorticoid and progesterone receptors. This compound has demonstrated minimal effects on intraocular pressure in preclinical studies, making it suitable for research into ocular pharmacology. The water-soluble formulation of Mifepristone methochloride is designed to enhance drug penetration in ocular tissues, facilitating studies on its therapeutic potential in eye diseases.
  46. Active Metabolite of EIDD-1723

    EIDD-036 is the active metabolite of EIDD-1723 and functions as a C-20 oxime derivative of Progesterone, with a notable binding affinity for the progesterone receptor (PR) demonstrated by an IC50 of 171 nM. This compound effectively penetrates the blood-brain barrier and is associated with potential therapeutic applications in acute trauma settings. EIDD-036 is specifically relevant for research in traumatic brain injury (TBI), aiding in the exploration of neuroprotective strategies following cerebral insult.
  47. Progestin

    Medrogestone is an orally active progestin that primarily targets progesterone receptors. It exhibits significant local progestational activity and effectively maintains pregnancy in ovariectomized rat models. Additionally, Medrogestone inhibits ovulation and serves as a method for pregnancy prevention. It has also been shown to significantly reduce the severity of benign prostatic hypertrophy, making it useful in various reproductive and therapeutic research applications.
  48. EIDD-036 Prodrug

    EIDD-1723 is a prodrug of EIDD-036, primarily targeting the progesterone receptor (PR) with an IC50 of 2.25 μM. This compound exhibits neuroprotective effects that may operate through both PR-dependent pathways and non-genomic mechanisms, including modulation of inflammatory responses and oxidative stress. EIDD-1723 is useful for investigating traumatic brain injury (TBI) and its potential therapeutic interventions.
  49. PGRMC2 Activator

    CPAG-1 is a small-molecule activator of the progesterone receptor membrane component 2 (PGRMC2). It enhances mitochondrial heme delivery to the nucleus, promoting the activation of genes associated with thermogenesis in brown adipose tissue, such as Ucp1 and Pgc-1α, while also decreasing lipid accumulation. Additionally, CPAG-1 has demonstrated the potential to lower fasting blood sugar and insulin levels, and improve glucose tolerance and insulin sensitivity. This compound is valuable for researching the mechanisms underlying type 2 diabetes.
  50. Progesterone Receptor Antagonist

    Onapristone is a potent progesterone receptor antagonist, exhibiting Kd values of 11.6 nM and 11.90 nM for the human endometrium and myometrium progesterone receptors, respectively. It demonstrates significant antitumor activity, making it valuable for research applications in oncology and reproductive biology. This compound is particularly useful for studies focused on the modulation of progesterone signaling pathways in the context of cancer and other related diseases.

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