Catalog No.
Product Name
Application
Product Information
Citations
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FSH Negative Allosteric Modulators
ADX68692 is a selective negative allosteric modulator of the follicle-stimulating hormone (FSH) receptor, exhibiting a log IC50 of -5.71. This compound effectively inhibits hCG-induced cAMP production and β-arrestin 2 recruitment in HEK293 cells. ADX68692 demonstrates partial efficacy in mLTC-1 and primary rat Leydig cells, leading to reduced FSHR-mediated cAMP, progesterone, and estradiol production. Additionally, it has been shown to decrease the number of oocytes recovered from the ampullae, making it a valuable tool for studying reproductive biology and hormonal regulation. -
Estrogen Derivative
J 628 is an estrogen derivative that primarily targets estrogen receptors. It exhibits antifertility effects and is utilized in research to explore reproductive health and associated mechanisms in animal models such as mice, rats, and rabbits. This compound serves as a valuable tool for investigating the physiological impacts of estrogen signaling and its implications for fertility regulation. -
Estrogen Receptor/ERR
RU-39411 is a steroidal anti-estrogen that targets the estrogen receptor (ERR) with mixed estrogenic and antiestrogenic properties. It demonstrates significant inhibitory effects on cell proliferation in the MCF-7 breast cancer model, linked to its binding affinity for the estrogen receptor. RU-39411 effectively downregulates the estrogen binding capacity in cells without altering estrogen receptor mRNA levels, suggesting that the incorporation of its side chain modifies typical steroidal estrogen antagonist behavior. Additionally, RU-39411 promotes the synthesis of progesterone receptors, supporting its role as an active estrogen. -
Estrogen Receptor Antagonist
Enclomiphene hydrochloride is a potent non-steroidal estrogen receptor antagonist. It exhibits antioestrogenic properties, making it valuable for research into ovarian dysfunction, testosterone deficiency, male hypogonadism, and type 2 diabetes. This compound's mechanism of action supports its use in exploring endocrine disorders and developing potential therapeutic strategies in related conditions. -
Estrogen Receptor Antagonist
4'-Raloxifene-β-D-glucopyranoside is a selective estrogen receptor antagonist, primarily targeting estrogen receptors to modulate their activity. This compound is a metabolite of Raloxifene and exhibits orally active properties, making it effective in research related to osteoporosis by inhibiting bone loss and resorption. Additionally, it has potential applications in studies focused on lipid metabolism and the management of lipid levels. -
Partial Anti-estrogen
Zindoxifene is a partial anti-estrogen that binds selectively to estrogen receptors, resulting in the inhibition of estrogen-dependent tumor cell growth. This compound exhibits both agonist and antagonist properties, making it useful for research into estrogen-dependent malignancies, including prostate and breast cancer. Its unique dual activity allows for versatile applications in the study of hormone-related cancer therapies. -
Estrogen Receptor Modulator
Levormeloxifene fumarate is a stable salt form of Levormeloxifene, functioning as an estrogen receptor modulator. It is particularly significant in the prevention of postmenopausal bone loss, demonstrating key biological activity in bone density preservation. This compound is of interest in research focused on osteoporosis and other estrogen-related conditions. -
Estrogen Receptor Antagonist
Estrogen Receptor Antagonist 8 functions as a potent antagonist of the estrogen receptor, exhibiting significant in vivo anti-uterotrophic activity with an EC50 of 4.160 μM. This compound is valuable for research applications aimed at understanding estrogen signaling pathways and developing hormone-related therapies. Its ability to inhibit estrogen receptor activity makes it a crucial tool in investigations of endocrine disruption and related biological processes. -
Estrogen Receptor Degrader
ER Degrader 12 is an estrogen receptor (ER) degrader with demonstrated IC50 values of 2.3 nM for ERα and 80.2 nM for ERβ, as shown in TR-FRET assays. This compound effectively inhibits the proliferation of MCF-7 breast cancer cells, exhibiting an IC50 of 1.53 nM. ER Degrader 12 is primarily utilized in research applications focused on understanding breast cancer biology and therapeutic strategies targeting estrogen signaling pathways. -
Estrogen Receptors Modulator
Psidial A is a selective estrogen receptor modulator derived from the epimer of a sesquiterpenoid-diphenylmethane meroterpenoid. This compound exhibits significant interactions with estrogen receptors, suggesting potential applications in cancer research, particularly in targeting estrogen-dependent pathways. Its unique structure and activity make it a valuable tool for investigating estrogen-mediated biological processes and therapeutic strategies in oncology. -
ERα/ERβ Antagonist
EM-800 is a potent antagonist of estrogen receptors α (ERα) and β (ERβ), exhibiting significant anti-estrogenic activity. This compound demonstrates anticancer properties by inhibiting the growth of breast cancer models induced by 7,12-Dimethylbenz[a]anthracene (DMBA). In ovariectomized animal studies, EM-800 effectively mitigates bone loss, presenting its utility in bone health research. Additionally, it offers valuable insights into breast and endometrial cancer studies, as well as potential benefits in lipid metabolism and overall metabolic health. -
Ovulation Induce
Clomifene hydrochloride is an orally active agent that primarily targets the hypothalamic estrogen receptors to induce ovulation. It is commonly employed in the treatment of female infertility by stimulating the release of gonadotropins, thereby promoting follicular development and ovulation. This compound is recognized for its relatively safe profile, ease of administration, and effectiveness in reproductive research applications. -
ERα Degrader
ERα Degrader 13 is a potent degrader of estrogen receptor alpha (ERα) with an IC50 value of 0.55 μM. This compound effectively induces tumor regression in breast cancer xenograft mouse models, making it a valuable tool for studying ERα-related signaling and therapeutic approaches in breast cancer. Its targeted degradation mechanism provides insights into the role of ERα in cancer progression and treatment resistance. -
ER Degrader
ER Degrader 13 is an estrogen receptor (ER) degrader that effectively induces the degradation of ER, thereby reducing its activity. This compound demonstrates a substantial inhibitory effect on the proliferation of estrogen receptor-positive breast cancer MCF-7 cells. ER Degrader 13 is utilized in research focused on targeted cancer therapies and mechanisms of hormone-driven cancers. -
Anti-estrogenic Agent
(E/Z)-Panomifene hydrochloride is a selective anti-estrogenic agent, functioning as an orally active analog of tamoxifen. This compound exhibits notable anti-tumor activity, making it a valuable tool in breast cancer research. Its mechanism of action primarily involves modulation of estrogen receptor pathways, supporting further studies into its therapeutic potential in oncology. -
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. -
FSH Receptor Agonist
TOP5300 is an orally active allosteric agonist of the follicle-stimulating hormone (FSH) receptor. This compound enhances testosterone production in stromal cells while promoting follicular genesis and superovulation in rat models. Its ability to modulate FSH receptor activity makes TOP5300 a valuable tool for investigating reproductive biology and potential therapeutic applications in fertility research. -
ER Antagonist
Estrogen receptor antagonist 3 functions primarily as an antagonist of the estrogen receptor (ER). By inhibiting estrogen signaling, it influences key biological processes such as cell growth, differentiation, and apoptosis. This compound holds potential for research applications in cancer diseases, providing a valuable tool for studying ER-mediated pathways in oncology. -
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. -
Antiosteoporotic Agent
BE-26263 is an antiosteoporotic agent derived from Scedosporium apiospermum, exhibiting estrogenic activity. This compound promotes bone health by mimicking the effects of estrogen, making it a valuable tool in osteoporosis research. Its application spans investigations into bone density regulation and potential therapeutic strategies for osteoporosis treatment. -
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. -
Anti-estrogen Deficiency Agent
LY88074 Methyl Ether is an anti-estrogen deficiency agent that acts by inhibiting estrogen deprivation pathways. This compound is effective in addressing various estrogen-deficient conditions, including osteoporosis and hyperlipidemia, thereby providing a potential therapeutic approach in managing estrogen-related disorders. Its application in research can aid in understanding the role of estrogen in disease processes and the development of targeted therapies. -
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 Modulator
Estrogen Receptor Modulator 11 is a tetrahydroisoquinoline derivative that selectively targets estrogen receptors (ER). It demonstrates affinity for both ERα and ERβ, with IC50 values of 285 nM and 421 nM, respectively. Notably, Estrogen Receptor Modulator 11 exhibits no antagonist activity in the MCF-7 cellular assay, indicating potential as a selective modulator in estrogen-related research applications. This compound is valuable for studies focused on ER signaling pathways and related therapeutic developments. -
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. -
FSH Receptor Antagonist
FSH Receptor Antagonist 1 specifically targets the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor, functioning as a potent antagonist with an IC50 of 28 nM in cells expressing this receptor. This compound effectively inhibits follicle development and ovulation in ex vivo mouse models, making it valuable for research in reproductive biology and hormonal regulation. Its application in studying FSH signaling pathways provides insight into fertility-related processes and potential therapeutic interventions. -
ERR Inhibitor
Millewanin G is a prenylated isoflavonoid that acts as an estrogen-related receptor (ERR) inhibitor, exhibiting antiestrogenic activity with an IC50 of 29 μM. This compound is primarily isolated from the leaves of M. pachycarpa, which is cultivated in Japan. Millewanin G is valuable for research applications focused on understanding ERR's role in various biological processes and its impact on diseases influenced by estrogen signaling. -
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. -
Estradiol Chemical Delivery System
E2-CDS (Estradiol 17-Dihydrotrigonelline) serves as a redox-based chemical delivery system for estradiol (E2). This compound enables sustained and selective delivery of estradiol to the brain, facilitating targeted research into its neurological effects. E2-CDS can be effectively utilized in studies investigating hormone-related processes and potential therapeutic applications in neurodegenerative disorders. -
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. -
ERRγ Inhibitor
ERRγ-IN-1 is a potent ERRγ inhibitor with an IC50 of 0.040 μM. It demonstrates activation of the MAPK (p44/p42) pathway while effectively inhibiting ERRγ activity. ERRγ-IN-1 has been shown to enhance iodine uptake in anaplastic thyroid carcinoma xenografts and to suppress tumor growth in nude mouse models. This compound is valuable for research focused on anaplastic thyroid carcinoma. -
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. -
ERβ Agonist
ERβ agonist-2 is a selective agonist for estrogen receptor beta (ERβ), exhibiting an EC50 of 800 nM or lower. It effectively inhibits T cell activation and proliferation, leading to a reduction in circulating T cell levels, while sparing neutrophils, monocytes, and B cells. This compound is relevant for research applications related to chronic heart failure post-myocardial infarction, as well as in studies of graft-versus-host disease, multiple sclerosis, and experimental autoimmune encephalomyelitis. -
Diethylstilbestrol precursor
Dimestrol is a diethylstilbestrol dimethyl ether precursor, primarily targeting estrogen receptors. It is utilized in biological research to investigate estrogen-related pathways and functions. Dimestrol serves as a valuable tool for studying hormonal interactions and developing therapeutic strategies in endocrine disturbances. -
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. -
(R,R)-THC Relative Configuration
rel-(R,R)-THC is an isomeric compound characterized by its distinct (R,R) configuration. It selectively acts as an agonist for estrogen receptor alpha (ERα) and as an antagonist for estrogen receptor beta (ERβ), exhibiting binding affinities with Ki values of 9.0 nM and 3.6 nM, respectively. This compound's higher binding affinity for ERβ compared to ERα, with values of 25 nM and 3.6 nM, positions it as a valuable tool for research into estrogen receptor modulation and related signaling 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. -
Estrogen Antagonist
D 15413 is an orally active nonsteroidal estrogen antagonist that effectively inhibits the growth of estrogen receptor-positive MCF-7 cells, achieving a 70% inhibition rate at a concentration of 10^-7 M. This compound demonstrates significant antitumor activity in models of breast cancer induced by DMBA and MNU, making it a valuable tool for research in breast cancer therapeutics and estrogen signaling pathways. -
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.
