Catalog No.
Product Name
Application
Product Information
Citations
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Androgen Receptor agonist
Cl-4AS-1 is a potent steroidal androgen receptor (AR) agonist with an IC50 of 12 nM. Additionally, it serves as an inhibitor of 5α-reductase types I and II, exhibiting IC50 values of 6 nM and 10 nM, respectively. This compound is valuable for studying androgen signaling pathways and investigating potential therapeutic applications in conditions related to androgen receptor modulation and steroid metabolism. -
Androgen Receptor Inhibitor
Androgen receptor-IN-6 is a potent inhibitor of the androgen receptor, specifically targeting the disordered N-terminal domain (NTD) with an in vitro IC50 of 0.12 μM. This compound demonstrates favorable membrane permeability in Caco2 cells and exhibits oral bioavailability in male CD-1 mice, with an F/% of 16%. It serves as a valuable tool for research into androgen receptor signaling pathways and the development of therapeutic strategies for androgen-dependent conditions. -
AR NTD Inhibitor
Ralaniten triacetate is an orally active inhibitor that targets the N-terminal domain (NTD) of the androgen receptor (AR). This first-in-class compound demonstrates efficacy against full-length androgen receptors as well as resistance-related variants, including AR-v7. It is primarily utilized in research focusing on androgen receptor signaling pathways and their role in hormone-driven cancers. -
Androgen Receptor Inhibitor
A4B17 is an androgen receptor N-terminal inhibitor that selectively targets the androgen receptor, interfering with its transcriptional activity. It is primarily used in research related to androgen-responsive prostate cancer, allowing for investigations into therapeutic strategies and mechanisms of resistance. A4B17 provides a valuable tool for studying androgen receptor signaling pathways and their implications in tumor progression. -
Stable Isotope
Darolutamide-d4 is a deuterium-labeled analog of Darolutamide, a competitive androgen receptor (AR) antagonist. It demonstrates a Ki of 11 nM for rat wild-type AR and an IC50 of 26 nM for human wild-type AR-mediated transcriptional activation, effectively inhibiting testosterone-induced AR nuclear translocation. This reagent selectively impacts AR-positive cells by disrupting AR-dependent signaling pathways, while its active metabolite retains full antagonistic activity against AR mutants. Darolutamide-d4 is valuable for research into prostate cancer, particularly in studies focused on androgen receptor-dependent mechanisms. -
AR Inhibitor
VPC-13566 is a selective inhibitor of the androgen receptor (AR), exerting its effects via inhibition of AR transcriptional activity. This compound effectively suppresses the proliferation of AR-dependent prostate cancer cell lines in vitro. VPC-13566 is a valuable tool for investigating the AR signaling pathway and identifying novel AR-interacting partners, making it relevant for cancer research applications. -
Nonsteroidal Androgen receptor Antagonist
BMS-641988 is a nonsteroidal androgen receptor antagonist that demonstrates a binding affinity with a Ki of 1.7 nM. This compound exhibits notable anticancer activity, making it valuable for research applications in oncology. Its ability to inhibit androgen receptor signaling positions BMS-641988 as a significant tool for exploring therapeutic strategies against androgen-dependent cancers. -
Stable Isotope
11-Ketodihydrotestosterone-d3 is a deuterium-labeled derivative of 11-Ketodihydrotestosterone, an endogenous steroid and active androgen. This compound acts as a potent agonist of the androgen receptor (AR), exhibiting a Ki value of 20.4 nM and an EC50 of 1.35 nM for human AR. It plays a significant role in the regulation of gene expression, protein synthesis, and cell proliferation in androgen-dependent prostate cancer research. 11-Ketodihydrotestosterone-d3 is valuable for metabolic studies and tracer applications in hormonal and cancer research. -
Androgen Receptor Inhibitor
Faznolutamide is an androgen receptor inhibitor that interferes with androgen signaling. This compound exhibits significant antiandrogenic activity, making it a valuable tool for investigating androgen-dependent biological processes. It is used in research focused on prostate cancer and other conditions influenced by androgens. -
SARM/AR Ligand
TFM-4AS-1 is a selective androgen receptor modulator (SARM) that acts as a potent androgen receptor (AR) ligand with an IC50 of 38 nM. This compound functions as a gene-selective agonist, making it valuable for studies focused on muscle wasting and bone density regulation. Its specificity provides a useful tool for exploring androgen receptor signaling pathways in various biological contexts. -
Stable Isotope
Linuron-d6 is a deuterated form of the phenylurea herbicide Linuron, which functions as a photosystem II inhibitor. This compound is primarily utilized in agricultural settings to effectively manage the growth of grass and weeds in crops and orchards. In addition to its herbicidal properties, Linuron exhibits activity as a competitive antagonist of the androgen receptor, with a Ki of 100 μM, and has been shown to induce reproductive toxicity in animal models, acting as an endocrine disruptor in research contexts. -
Androgen Receptor Antagonist
6-Amino-5-bromoquinoxaline is an androgen receptor antagonist that functions through selective inhibition of androgen receptor activity. This compound is noted for its potential applications in research related to hormone signaling pathways and the investigation of androgen-related disorders. Its utility may extend to studies involving prostate cancer and other androgen-sensitive conditions. -
Anti-androgen
SK33 is a trifluoromethylated enobosarm analog that functions as a potent and tissue-selective anti-androgen. It effectively reduces androgen receptor (AR) transcriptional activity, making it a valuable tool for studying androgen-related signaling pathways. This compound is particularly relevant for research in prostate cancer and other androgen-dependent disorders. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 9 is a selective antagonist of the androgen receptor, inhibiting its activity in cellular contexts. This compound is primarily utilized in research focusing on androgen signaling pathways, offering insights into prostate cancer and other androgen-related diseases. Additionally, it contributes to studies aimed at understanding the role of androgens in various physiological processes and conditions. -
Androgen Receptor Modulator
LGD-2226 is a selective androgen receptor modulator (SARM) with high potency, exhibiting an EC50 of 0.2 nM and a Ki of 1.5 nM for the human androgen receptor. It demonstrates tissue selectivity, showing diminished effects on prostate tissue relative to muscle in in vivo models. Researchers can utilize LGD-2226 in studies related to muscle wasting, osteoporosis, and sexual dysfunction to explore therapeutic strategies targeting androgen receptors. -
Androgen Receptor Modulator
GLPG0492 (R enantiomer) is a selective androgen receptor modulator that exhibits significant affinity for the androgen receptor. This compound demonstrates potential for promoting anabolic effects in muscle and bone, making it a valuable tool for research in androgen signaling and related therapeutic applications. Its specificity may provide insights into the mechanisms of androgen action and the development of novel treatments for conditions related to androgen deficiency. -
Antiandrogen/Antitumor Agent
Gridegalutamide is an antiandrogen that functions by inhibiting androgen receptor signaling, contributing to its antitumor effects. This compound is primarily utilized in research focused on prostate cancer and other androgen-sensitive malignancies, making it valuable for investigating therapeutic strategies targeting the androgen receptor pathway. -
Anabolic Androgenic Steroid Metabolite
19-Noretiocholanolone is a metabolite of the anabolic androgenic steroid Nandrolone, functioning primarily as an androgen receptor agonist. This compound exhibits significant anabolic activity, promoting muscle growth and strength enhancement. It is commonly used in research applications focused on the effects of anabolic steroids and their metabolic byproducts on physiological processes. -
Androgen Receptor Antagonist
(Rac)-PF-998425 is a potent, selective nonsteroidal antagonist of the androgen receptor (AR). It exhibits IC50 values of 26 nM in AR binding assays and 90 nM in cellular assays, demonstrating significant efficacy in inhibiting AR activity. This compound is particularly relevant for research applications in androgenetic alopecia and related androgen-mediated conditions. -
AR Antagonist
Apalutamide-d4 is a deuterium-labeled derivative of Apalutamide, functioning as a potent competitive antagonist of the androgen receptor (AR). It demonstrates a binding affinity with an IC50 of 16 nM, making it valuable for studies involving androgen signaling pathways. This reagent is primarily used in research applications focused on prostate cancer and androgen-related disorders, facilitating the investigation of AR-mediated mechanisms and potential therapeutic strategies. -
Stable Isotope
Apalutamide-d3 is a deuterium-labeled derivative of Apalutamide, a highly selective androgen receptor (AR) antagonist with an IC50 of 16 nM. This stable isotope is designed for applications in pharmacokinetic studies and metabolic profiling, facilitating the investigation of AR signaling pathways and the pharmacodynamics of AR-targeted therapies in various models. Its use in research enables precise tracking and quantification in biological systems, enhancing our understanding of androgen receptor modulation in cancer therapies. -
AR Antagonist
AR Antagonist 3 is a selective androgen receptor (AR) antagonist with a measured IC50 of 0.47 µM, demonstrating strong potency in blocking AR activity. It effectively reduces FRET signal in a dose-dependent manner, with an IC50 of 18.05 μM. In preclinical studies, AR Antagonist 3 has shown significant inhibition of tumor growth upon intratumoral administration, making it a valuable tool for research in androgen receptor-related cancer therapies. -
AR Antagonist
Galloylalbiflorin is an androgen receptor (AR) antagonist with an IC50 of 53.3 μM, isolated from the roots of Paeonia lactiflora. This compound demonstrates notable anti-androgenic activity, making it valuable for research related to androgen signaling pathways and its implications in diseases such as prostate cancer. It serves as a useful tool for investigating AR-related biological processes and therapeutic applications in hormone-related disorders. -
Stable Isotope
Ostarine-d4 is a deuterated form of Ostarine, primarily functioning as a stable isotope. This labeled compound is utilized in pharmacokinetic studies, enabling accurate tracking of Ostarine metabolism and distribution within biological systems. Its application is critical for research on selective androgen receptor modulators and their effects on muscle and bone metabolism. -
Androgen Receptor
Trestolone is a synthetic anabolic-androgenic steroid that primarily targets the androgen receptor. It exhibits significant anabolic activity, promoting muscle growth and development while also enhancing physical performance. Trestolone is commonly utilized in research applications focused on muscle physiology, testosterone effects, and various anabolic processes. -
Androgen Receptor Modulator
GTx-027 is a selective androgen receptor modulator (SARM) that exhibits potent transactivation of the androgen receptor (AR) with an EC50 of 1.8 nM. This non-steroidal compound selectively promotes anabolic processes, leading to increased muscle weight while sparing androgenic effects on secondary sexual organs. GTx-027 is primarily utilized in research related to breast cancer and stress urinary incontinence (SUI). -
Androgen Receptor Antagonist
PF-998425 is a selective nonsteroidal androgen receptor (AR) antagonist, demonstrating significant potency with an IC50 of 37 nM in AR binding assays and 43 nM in cellular assays. This compound exhibits minimal activity towards common receptors and enzymes, such as the progesterone receptor. PF-998425 is relevant for research applications involving sebum control and the investigation of androgenetic alopecia. -
NSAA
RD162 is a diarylthiohydantoin and a non-steroidal antiandrogen (NSAA) that exhibits selective binding to the androgen receptor (AR). This compound is notable for its ability to induce tumor regression in mouse models of castration-resistant human prostate cancer, highlighting its potential as a therapeutic agent in prostate cancer research. RD162 serves as a valuable tool for studying AR-targeted therapies and the mechanisms underlying castration resistance in prostate malignancies. -
Anti-Androgenic Agent
N-Nitrosodicyclohexylamine (NDCHA) is an N-nitroso compound known for its anti-androgenic properties. It acts as a competitive antagonist of the androgen receptor (AR), effectively inhibiting the binding of 5α-dihydrotestosterone. Additionally, NDCHA reduces the protein levels of AR, making it a valuable tool for investigating androgen signaling pathways and potential therapeutic targets in androgen-related disorders. -
Androgen Receptor Inhibitor
Bifluranol is an androgen receptor inhibitor that functions by blocking the action of androgens, which are hormones that can promote the growth of certain cancers. This compound exhibits anti-androgenic activity, making it valuable in research addressing hormone-dependent cancers, such as prostate cancer. Bifluranol can be utilized in studies focused on understanding androgen signaling pathways and developing therapeutic strategies targeting androgen-related conditions. -
AR Modulator
TLB 150 Benzoate is an androgen receptor modulator that demonstrates a potent activity with an IC50 of 0.13 μM. This compound is designed for research applications focused on androgen signaling pathways and may provide insights into steroid receptor biology. It is suitable for investigating the modulation of androgen receptor activity in various cellular models. -
3β-androstanediol Analog
Apoptone is a 3β-androstanediol analog that primarily targets the androgen receptor. This compound is known to reduce the expression of the androgen receptor and decrease intratumoral androgen levels. Apoptone demonstrates significant anticancer activity, particularly against castration-resistant prostate cancer, making it a valuable tool for cancer research and therapeutic studies. -
Stable Isotope
Nilutamide-d6 is a deuterium-labeled derivative of Nilutamide, a non-steroidal anti-androgen agent primarily targeting androgen receptors. This stable isotope is utilized in metabolic studies and pharmacokinetic research of Nilutamide, particularly in the context of metastatic prostate carcinoma. Its precise labeling allows for enhanced tracking and quantification of drug metabolism and efficacy in various biological systems. -
Anti-Androgen Agent
Chlormadinone is an anti-androgen agent that acts by inhibiting androgen receptors. This compound is primarily used in the research of benign prostatic hyperplasia (BPH), as it modulates testosterone activity and can influence prostate growth and function. Its application extends to the investigation of hormonal regulation in various prostate conditions. -
Anabolic Androgenic Steroid
6α-Chloro testosterone is an anabolic androgenic steroid that functions primarily through androgen receptor modulation. It exhibits significant anabolic activity, promoting muscle growth and enhancing physical performance. This compound is utilized in research involving androgenic effects, muscle metabolism, and hormonal studies in both in vitro and in vivo models. -
Thiohydantoin Derivative
CH4933468 is a thiohydantoin derivative that functions as a pure antagonist of the androgen receptor (AR). This compound effectively inhibits AR-mediated transactivation and suppresses the proliferation of LNCaP and LNCaP-BC2 cancer cell lines. CH4933468 is particularly relevant for research in castration-resistant prostate cancer (CRPC), providing a valuable tool for investigating therapeutic strategies in this context. -
Androgen receptor Inhibitor
Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor, demonstrating significant anticancer activity. This compound also disrupts the production of pro-inflammatory cytokines, including IL-17A, IL-17F, and IFN-γ, making it a valuable tool for studying androgen receptor signaling and its role in cancer and immune responses. Its multifaceted activity positions Androgen receptor-IN-5 as a promising candidate for research in cancer therapeutics and inflammation modulation. -
Anti-Cancer Agent
WCA-814 is a conjugate that functions as an androgen receptor (AR) antagonist and Hsp90 inhibitor. This compound effectively induces degradation of full-length androgen receptors as well as the AR-V7 variant. WCA-814 demonstrates notable cytotoxicity in prostate cancer cells, with an IC50 of 171.2 nM, and 26.5 nM and 22 nM for LNCaP and 22Rv1 cell lines, respectively. This makes it a valuable tool for research in prostate cancer therapeutics and underlying mechanisms of androgen receptor signaling. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 7 is a potent antagonist of the androgen receptor (AR) with an IC50 value of 1.18 µM. This compound demonstrates biological activity in vitro, effectively inhibiting the expression of AR target genes in a dose- and time-dependent manner, with a GI50 of 7.9 µM. It is primarily used in research related to androgen signaling pathways and may aid in studies of hormone-driven diseases, such as prostate cancer. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 10 is a selective antagonist of the androgen receptor, a key target in the modulation of androgen-related biological processes. This compound effectively reduces wax ester accumulation in the golden Syrian hamster model, demonstrating its potential utility in studies related to lipid metabolism and hormonal regulation. Its application in research may extend to exploring androgen receptor signaling pathways and their implications in metabolic disorders. -
Androgen Antagonist
Gumelutamide monosuccinate is an androgen antagonist that functions primarily by inhibiting androgen receptor signaling. This tetrahydropyridopyrimidine compound exhibits notable antineoplastic activity, making it relevant for research in cancer treatment, particularly in hormone-sensitive tumors. Its mechanism of action facilitates investigations into therapeutic strategies aimed at disrupting androgen-driven pathways in oncology. -
Androgenic Compound
Androstatrione is an androgenic compound that primarily targets androgen receptors. It exhibits significant biological activity by modulating androgen-dependent pathways, making it valuable for research in hormonal regulation and potential therapeutic applications in prostate cancer and androgen-related disorders. Additionally, it can be utilized in studies investigating the effects of androgens on cell proliferation and differentiation. -
Endogenous Metabolite
Estromustine is the active metabolite of Estramustine phosphate, primarily targeting the mutant androgen receptor (m-AR). It demonstrates an EC50 of 2.6 μM in LNCaP prostate cancer cells and exhibits cytotoxicity with an IC50 of 9.73 μM. This compound is valuable for research focused on androgen receptor mutations and their role in prostate cancer therapeutics. -
Androgen Receptor Ligand/Estrogen Receptor Agonist
4-sec-Butylphenol is an androgen receptor ligand, exhibiting a binding affinity with a pIC50 value of 4.07. Additionally, it acts as an estrogen receptor agonist, contributing to its significant biological activity. This compound is commonly detected in industrial effluents and production water from oil and gas extraction, as well as in samples from river water, making it relevant for environmental research and toxicology studies. -
Androgen Receptor Antagonist
Androgen Receptor Antagonist 13 is an orally active antagonist of the androgen receptor, exhibiting an IC50 of 0.20 μM. This compound is particularly relevant in prostate cancer research, serving as a valuable tool for studying androgen signaling pathways and potential therapeutic interventions in androgen-dependent malignancies. -
Stable Isotope
Flutamide-d7 is a deuterated form of Flutamide, serving as a stable isotope used in metabolic and pharmacokinetic studies. This compound is instrumental in tracing the metabolic pathways of Flutamide, enhancing the understanding of its pharmacodynamics and pharmacokinetics. Flutamide-d7 is primarily applied in research focused on androgen receptor modulation and anti-androgen therapies. -
AR Antagonist
(–)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). It demonstrates superior potency compared to its enantiomer, inhibiting androgen-induced AR activity and exhibiting a distinct mechanism of action that differs from Enzalutamide. (–)-JJ-450 effectively reduces the transcriptional activity of both wild-type AR and the mutant ARF876L by preventing AR nuclear translocation and facilitating the nuclear degradation of unbound AR. This compound is particularly relevant for research into castration-resistant prostate cancer (CRPC) that shows resistance to Enzalutamide. -
Antiandrogen Agent
Bicalutamide sulfide is a nonsteroidal antiandrogen agent that targets androgen receptors to inhibit androgen activity. It demonstrates significant biological activity in the study of androgen-responsive benign and malignant diseases. This compound is useful for research applications involving prostate cancer and other conditions influenced by androgens. -
AR Degrader/CYP17A1 Inhibitor
YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context. -
AR Antagonist
BMS-779333 is an orally active antagonist of the androgen receptor (AR). This compound demonstrates potential in the research of prostate cancer by inhibiting AR-mediated signaling pathways, thus implicating it in the modulation of tumor growth. Additionally, BMS-779333 may play a role in exploring therapeutic approaches for seizure disorders.
