Catalog No.
Product Name
Application
Product Information
Citations
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Estrogen Receptor Antagonist
Etacstil is a selective estrogen receptor antagonist known for its minimal uterotropic activity in ovariectomized rats. By inhibiting the agonist effects of estradiol, tamoxifen, and raloxifene, Etacstil serves as a valuable tool for investigating mechanisms in breast cancer and bone protection research. Its unique profile makes it ideal for studying estrogen receptor modulation in various biological contexts. -
Estrogen Receptor α Antagonis
Estrogen Receptor α Antagonist 1 is a highly selective antagonist specifically targeting the estrogen receptor α (ERα), displaying IC50 values of 0.02 μM for ERα, 6.55 μM for estrogen receptor β, and 7.73 μM for MCF-7 cells. This compound offers significant potential for research applications in cancer biology, particularly in studies focusing on estrogen signaling pathways and their involvement in malignancies. Its selectivity makes it a valuable tool for investigating the role of ERα in cancer progression and therapy. -
Estrogen Receptor/ERR
(E,E)-GLL398 is a selective estrogen receptor degrader that exhibits strong binding affinity for estrogen receptor alpha (ERα) with an IC50 of 1.14 nM. This compound is capable of effectively degrading ERα in MCF-7 breast cancer cells, demonstrating an IC50 of 0.21 μM. The incorporation of a boronic acid moiety enhances its oral bioavailability, achieving an AUC of 36.9 μg·h/mL in rat models, supporting its potential for therapeutic applications in hormone-dependent cancers. -
Estrogen Receptor Modulator
HMR-3339 is a selective estrogen receptor modulator that demonstrates significant effects on lipid metabolism by reducing total cholesterol, low-density lipoprotein cholesterol, and homocysteine levels. Additionally, HMR-3339 exhibits the ability to correct bone alterations induced by ovariectomy, making it a valuable tool for research in osteoporosis and cardiovascular health. Its diverse biological activities position it as a key reagent for studying estrogen receptor signaling and its effects on bone and lipid profile regulation. -
Estrogen Receptor Modulator
CHF 4227 free base is a selective estrogen receptor modulator (SERM) that exhibits high affinity for both human estrogen receptor-α and -β, with Ki values of 0.017 nM and 0.099 nM, respectively. This compound demonstrates significant biological activity in modulating estrogen-related pathways, making it valuable for research in hormone-dependent tumors and other estrogen-related diseases. Its oral bioavailability allows for convenient administration in various preclinical studies. -
Estrogen Receptor Regulator
Icariside D1 is a flavonoid glycoside that acts as a regulator of estrogen receptors. This compound exhibits antioxidant and anti-inflammatory properties, making it valuable for research in osteoporosis, male infertility, female reproductive dysfunction, and certain cancers. Its ability to modulate estrogen signaling positions Icariside D1 as a significant candidate for studies exploring hormone-related conditions. -
Antiestrogenic Compound
Anordiol is an antiestrogenic compound that exhibits weak estrogenic activity. It has been shown to mitigate parameters of uterine growth, such as wet weight, soluble protein, and DNA content, in estradiol-induced rat models. Additionally, Anordiol can modulate the estrous cycle in rats, indicating its potential utility in the research of antiestrogen-related diseases. -
Estrogen Receptor Ligand
CMP8 is a selective ligand for the estrogen receptor, specifically targeting the mutant estrogen receptor ligand binding domain (ERLBD). This compound demonstrates potent biological activity with IC50 values of 29 nM for MGERα, 41 nM for MGRERα, 1100 nM for human ERα, and 2200 nM for human ERβ. CMP8 is valuable for research applications focused on estrogen receptor modulation and its role in cancer biology. -
Estrogen Receptor (ER) Activator
Estrone acetate is an estrogen derivative that acts as an estrogen receptor (ER) activator. It promotes mammary gland development, stimulates prolactin secretion from the pituitary, and induces the proliferation and activation of lactotrophs, which is evidenced by alterations in organelle morphology. This compound is valuable for endocrine research, particularly in the exploration of estrogen’s role in pituitary function, prolactin regulation, and mammary tumor models. -
ER Degrader
ER Degrader 1 is a highly effective compound targeting the estrogen receptor (ER) for degradation. By modulating the estrogen signaling pathway, this reagent plays a crucial role in regulating cellular processes such as growth, differentiation, and apoptosis. ER Degrader 1 is valuable for investigating the mechanisms underlying cancer biology and developing potential therapeutic strategies for estrogen-dependent tumors. -
Estrogen Receptor/ERR Modulator
Estrogen Receptor Modulator 12 is a selective estrogen receptor modulator (SERM) targeting estrogen receptors with both agonist and antagonist properties. In vivo studies demonstrate its antagonistic effects on uterine tissue while promoting estrogenic activity in bone, plasma lipid profiles, and alleviating postmenopausal symptoms such as hot flashes and vaginal atrophy. Due to its dual functionality, this compound is a promising candidate for therapeutic applications in managing postmenopausal conditions. -
Estrogen Receptor Degrader
LX-039 is a potent and selective estrogen receptor degrader with an EC50 value of 2.29 nM. Featuring an indole C-3 chlorine substituent, LX-039 demonstrates favorable pharmacokinetics in mouse models, characterized by low clearance and high maximum concentration (Cmax) following oral administration. Its efficacy in degrading estrogen receptors highlights its potential for anti-tumor applications in research settings. -
ER Degrader
ER Degrader 3 is a potent agent that targets and degrades the estrogen receptor (ER). By disrupting the estrogen signaling pathway, this compound can influence critical biological processes such as cell growth, differentiation, and apoptosis. ER Degrader 3 is suitable for research applications focused on cancer biology, particularly in studies aimed at understanding estrogen-mediated tumorigenesis and therapeutic strategies. -
Target of Estrogen Receptor 1
Inokosterone is a compound that targets Estrogen Receptor 1, providing potential therapeutic benefits in rheumatoid arthritis. Its modulation of estrogen signaling may play a crucial role in alleviating inflammatory responses associated with the condition. This compound is of interest for research applications focusing on autoimmune disorders and endocrine regulation. -
Estrogen Receptor/ERR Agonist
Rel-Erteberel is a potent and selective agonist of the estrogen receptor beta (ERβ), exhibiting a Ki of 1.54 nM and an EC50 of 3.61 nM. This compound demonstrates significant anti-tumor activities, making it a valuable tool in cancer research. Its targeted mechanism allows for further exploration in studies of estrogen signaling pathways and their roles in various tumors. -
ERα Degrader
ER Degrader 6 is a potent degrader of Estrogen Receptor alpha (ERα). This compound disrupts the microtubule network by inhibiting tubulin polymerization, leading to effective tumor growth suppression. It demonstrates significant efficacy in preclinical models, making it a valuable tool for research on ERα-related cancers and therapeutic strategies targeting estrogen signaling pathways. -
Estrogen Receptor Modulator
Levormeloxifene is a selective estrogen receptor modulator (SERM) primarily targeting estrogen receptors to prevent and mitigate postmenopausal osteoporosis. This compound exhibits significant biological activity in bone metabolism, promoting bone density and reducing fracture risk in postmenopausal women. Additionally, Levormeloxifene has been associated with various adverse gynecological effects, highlighting its complex pharmacological profile and relevance in estrogen-related research applications. -
Estrogen Receptors Ligand
Hexolame is an estrogen receptor agonist that exhibits dual anticoagulant and estrogenic activities. By binding to estrogen receptors, Hexolame modulates clotting factors and platelet activity, leading to its anticoagulant effects. This compound is valuable for research focused on prostatic cancer and the prevention of thrombosis, offering insights into therapeutic strategies targeting these conditions. -
Estrogen Receptor/ERR Modulator
Zuclomiphene is an estrogen receptor modulator that exhibits antiestrogenic properties. This compound is known for its oral bioactivity and has been shown to reduce cholesterol levels. Research applications for Zuclomiphene include studies in endocrinology and metabolic diseases, making it a valuable tool for investigating hormonal regulation and metabolic pathways. -
ER Degrader
ER Degrader 5 is a potent estrogen receptor (ER) degrader that promotes the degradation of the ER, leading to decreased estrogen signaling. This compound exhibits significant anti-proliferative activity in estrogen-responsive breast cancer cells. ER Degrader 5 is an essential reagent for researchers investigating breast cancer mechanisms and the potential therapeutic effects of targeting ER pathways. -
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. -
Estrogen Receptor Modulator
Arzoxifene is a selective estrogen receptor modulator (SERM) that exhibits significant antiestrogenic effects on breast cancer and the endometrium, while simultaneously promoting favorable estrogenic activities on bone density and lipid profiles. This orally active compound possesses a fixed ring structure similar to raloxifene, minimizing side effects associated with estrogenic modulation. Arzoxifene is a valuable tool for investigating estrogen-related pathways and therapeutic strategies in hormone-responsive cancers and related disorders. -
Estrogen Receptor Antagonist
Nafoxidine hydrochloride is a non-steroidal estrogen receptor antagonist that exhibits potent antitumor activity in breast cancer models. This compound effectively inhibits estrogen-dependent cell proliferation, making it a valuable tool for investigating estrogen signaling pathways and therapeutic strategies in hormone-sensitive tumors. Its application in research provides insights into the role of estrogen receptors in cancer biology and potential treatment options for breast cancer patients. -
Estrogen Receptor/ERR Activator
(+)‐Medicarpin is a pterocarpan isoflavonoid that acts as an activator of the estrogen receptor (ER) β pathway. This compound inhibits osteoclastogenesis, thereby promoting bone healing and increasing bone mass through enhanced osteoblast differentiation. Its biological activities make it a valuable reagent for research applications focused on bone biology and estrogen signaling. -
ER Degrader
ER Degrader 11 is a selective estrogen receptor (ER) degrader that exhibits high potency with an IC50 of 1.6 nM for ERα. This compound is characterized by its oral bioavailability and ability to penetrate the blood-brain barrier, making it an important tool for investigating the mechanisms underlying breast cancer brain metastasis. Its targeted action on estrogen receptors positions ER Degrader 11 as a valuable reagent for cancer research and therapeutic studies. -
Estrogen Receptor α Antagonist
Raloxifene 4-Monomethyl Ether is an antagonist of the estrogen receptor α. This compound demonstrates significant biological activity by inhibiting MCF-7 breast cancer cells, with an IC50 value of 1 μM and a pIC50 of 6. It serves as a valuable tool for research applications related to estrogen signaling and breast cancer therapeutics. -
Antiestrogen
Mepitiostane is an orally active steroidal antiestrogen that inhibits estrogen receptor activity. This compound demonstrates potential biological activity in the research of breast cancer, making it valuable for studies aimed at understanding estrogen-related tumorigenesis and therapeutic interventions. Its unique mechanism allows for the exploration of antiestrogen properties in various cancer models. -
Selective Estrogen Receptor Modulator
NKS-01 is a selective estrogen receptor modulator (SERM) that exhibits targeted activity on estrogen receptors. This compound is primarily utilized in cancer research, specifically in the study of estrogen receptor-positive breast cancer, where it may influence tumor growth and proliferation. Its ability to selectively modulate estrogen receptor activity makes it a valuable tool for investigating therapeutic strategies in hormone-related malignancies. -
Estrogen Receptor Modulator
SR 16234, a selective estrogen receptor modulator, targets estrogen receptors to exert its biological effects. This compound has shown promise in the research of pain symptoms associated with endometriosis, making it a valuable tool for studies investigating the role of estrogen modulation in pain management. Its specific activity provides insights into the underlying mechanisms of endometriosis-related discomfort. -
Estrogen Receptor/ERR Agonist
WAY-214156 is a synthetic nonsteroidal compound that selectively agonizes the estrogen receptor beta (ERβ). It has been shown to exhibit robust biological activity, impacting various signaling pathways associated with estrogenic effects. This compound is valuable for research applications focusing on hormone signaling, endocrine regulation, and potential therapeutic strategies targeting ERβ-related disorders. -
Estrogen Receptor Agonist
Dehydrodiconiferyl alcohol is an estrogen receptor agonist that plays a significant role in promoting BMP-2-induced osteoblastogenesis. Additionally, this compound exhibits anti-inflammatory properties by inactivating NF-κB pathways. It is relevant for research in bone metabolism and inflammatory response modulation. -
Estrogen Receptor Inhibitor
Yp537 is an estrogen receptor inhibitor that disrupts the dimerization of the human estrogen receptor. This action effectively impedes estrogen-mediated signaling pathways, making it valuable for research on hormone-dependent cancers and other estrogen-related diseases. Yp537 is suitable for studying the molecular mechanisms underlying estrogen receptor activity and evaluating potential therapeutic strategies targeting these pathways. -
Estrogen Receptor Ligand
Ent-Estradiol is a selective ligand for the estrogen receptors, specifically targeting both ERα and ERβ. As the enantiomer of 17β-Estradiol, it exhibits minimal estrogenic activity, making it valuable for studies that require the modulation of estrogen receptors without significant hormonal effects. Ent-Estradiol demonstrates varying inhibitory concentrations with IC50 values of 24.9 nM, 9.59 nM, and 8.17 nM for human, rat, and mouse ERβ, respectively, and 151 nM, 246 nM, and 268 nM for ERα across the same species. This compound is instrumental in researching menopausal physiological changes and receptor-specific mechanisms. -
ERα Degrader
(1S,3R)-GNE-502 is a selective estrogen receptor alpha (ERα) degrader, exhibiting a potent EC50 of 13 nM in MCF7 human breast cancer cells. This compound effectively downregulates ERα levels, making it a valuable tool for investigating estrogen-mediated signaling pathways in cancer research. Its application extends to exploring therapeutic strategies for ERα-positive breast cancer and understanding the biological mechanisms underlying estrogen receptor regulation. -
GPER Agonist
CITFA is a GPER agonist that stimulates the G-protein coupled estrogen receptor. This compound has demonstrated the ability to promote neurite growth in hippocampal neurons derived from rat embryos (E18), making it a valuable tool for studying neuronal development and the effects of estrogenic signaling in neurobiology. Its application may extend to research on neuroprotection and neurodegenerative diseases. -
Estrogen Receptor Antagonist
Estrogen receptor antagonist 5 is a potent inhibitor of the estrogen receptor, a transcriptional regulatory protein that modulates various biological responses through its binding with endogenous estrogens. This compound is valuable for research related to metastatic disease, providing insights into its mechanisms and potential therapeutic targets. It serves as a critical tool for studies investigating estrogen signaling pathways and their role in cancer progression. -
ERα Degrader
PSDalpha is an estrogen receptor alpha (ERα) degrader that features a conjugation of a photosensitizer (PS), triphenylamine benzothiadiazole (TB), and 17β-estradiol through an acetylene bond. It demonstrates potent anti-proliferative effects on MCF-7 breast cancer cells. PSDalpha exhibits a maximum absorption wavelength of 465 nm in the visible spectrum, making it suitable for photodynamic therapy applications and studies related to ERα-targeted cancer treatments. -
Estrogen Receptor β Agonist
Estrogen Receptor Modulator 6 is a selective agonist for Estrogen Receptor β, demonstrating a Ki value of 0.44 nM. With a 19-fold selectivity for ERβ over ERα (Ki = 8.4 nM), this compound enhances ERβ-mediated signaling, making it a valuable tool for studies in estrogen signaling pathways and related therapeutic research. Its selective action positions it as a potential candidate for investigating disorders influenced by estrogen receptor activity. -
Estrogen Receptor Antagonist
Estrogen receptor antagonist 6 acts as a potent antagonist of the estrogen receptor, a ligand-activated transcriptional regulatory protein implicated in various biological processes mediated through endogenous estrogens. This compound is valuable for research applications focusing on metastatic disease, as it can effectively disrupt estrogen signaling pathways. Its use may facilitate investigations into the role of estrogen receptors in cancer progression and treatment resistance. -
Estrogen Receptors Antagonist
Estrogen Receptor Antagonist 7 is a potent inhibitor of estrogen receptors (ER), demonstrating significant antiproliferative activity in breast and ovarian cancer cells. This compound exhibits anticancer and anti-uterotrophic activities, making it a valuable reagent for research focused on estrogen-mediated signaling pathways and related oncological studies. Its applications extend to investigating the role of estrogen in cancer cell biology, as well as potential therapeutics targeting estrogen-dependent tumors. -
Estrogen Receptor Degrader
ER Degrader 4 is a selective estrogen receptor degrader (SERD) that operates through degradation of the estrogen receptor. This compound exhibits significant anti-tumor activity, making it valuable in research focused on estrogen-dependent cancers. Its oral bioavailability enhances its utility in preclinical studies exploring therapeutic strategies for breast cancer and other estrogen-related malignancies. -
Estrogen Receptor/ERR
Stilbestrol dipropionate is a synthetic estrogenic compound that primarily targets the estrogen receptor (ERR). It exhibits hormone-suppressive activity relevant for the treatment of recurrent prostate cancer. Additionally, Stilbestrol dipropionate can be utilized in a range of research applications focused on conditions associated with estrogen deficiency, making it a valuable tool for studying hormone-related pathways in various biological contexts. -
Antiestrogen
RU58668 is a steroidal antiestrogen that inhibits estrogen receptor activity, making it a powerful antiproliferative agent in hormone-sensitive breast cancer models such as MCF-7 cells. This compound is primarily utilized in research applications focused on breast cancer biology and the mechanistic study of antiestrogen therapies. Its ability to modulate estrogen signaling pathways provides valuable insights into the development of therapeutic strategies against estrogen receptor-positive tumors. -
Estrogen Receptor/ERR Antagonist
ERRγ Inverse Agonist 1 is a selective inverse agonist of the estrogen-related receptor gamma (ERRγ) with an IC50 value of 40 nM. This compound exhibits potent antagonistic activity, making it useful for investigating the role of ERRγ in various biological processes. It is particularly relevant for research applications focused on metabolic regulation and cancer biology, where modulation of ERRγ signaling is of interest. -
Estrogen Receptor Partial Agonist
Geranium oil functions as a partial agonist of the estrogen receptor (ER), promoting enhanced cytotoxicity in the presence of Tamoxifen (TMX) in GT1-7 cells. Its mechanism indicates potential for investigating the neurotoxic effects of TMX on the central nervous system. This compound is valuable for research related to neurological disorders, including dementia, offering insights into the interplay between estrogen signaling and neurodegenerative processes. -
ER Agonist
TTC-352 is an orally bioavailable selective partial agonist of the human estrogen receptor (ER) α, classified as a ShERPA. It effectively inhibits the proliferation of estrogen receptor-positive breast cancer cells, demonstrating significant antitumor activity. Additionally, TTC-352 promotes tumor regression by facilitating the translocation of ERα from the nucleus to extranuclear locations, making it a valuable tool for research in breast cancer therapeutics. -
Estrogen Receptor/ERR Activator
Phenolphthalol is an estrogen receptor (ER) activator known for its laxative properties. It demonstrates estrogenic activity and can influence various biological pathways related to estrogen signaling. This compound is primarily utilized in research applications investigating hormonal regulation, receptor activity, and relevant pharmacological studies. -
ER Agonist
17-Epiestriol is an estrogen metabolite that acts as a selective estrogen receptor (ER) β agonist. It is known to inhibit the mRNA and protein expression of vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα), thereby preventing NF-κB migration to the nucleus. Additionally, 17-epiestriol promotes the expression of endothelial nitric oxide synthase at both mRNA and protein levels. This compound is useful in research related to vascular inflammation and endothelial function. -
Estrogen Receptor/ERR
Lactandrate targets the estrogen receptor alpha (ERα) as a D-high nitrogen steroid alkylating agent. It exhibits a significant growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. In vivo studies have demonstrated its anti-tumor activity in mouse models of breast cancer, including MXT and CD8F1 strain tumors, as well as in human xenograft MX-1 models. Lactandrate serves as a valuable reagent for research in cancer biology, particularly in studying estrogen receptor modulation and breast cancer therapeutics. -
Estrogen Receptor Anolog
10-Chloroestra-1,4-diene-3,17-dione is an analog of the estrogen receptor, primarily targeting this pathway to modulate estrogenic activity. This compound demonstrates significant biological activity in studies involving hormone-related signaling and receptor interactions. It is commonly utilized in research applications focused on endocrine modulation, cancer biology, and the exploration of estrogen-related mechanisms in cellular processes.
