Androgen Receptors

Zanoterone is an orally active antagonist of the androgen receptor (AR), exhibiting a Ki of 2.2 μM. By inhibiting the binding of androgens, including testosterone and dihydrotestosterone (DHT), Zanoterone effectively disrupts the androgen signaling pathway. This action is significant for reducing androgen-dependent conditions such as prostate hyperplasia and prostate cancer growth, making it a valuable tool in androgen-related research and therapeutic development.

Inocoterone acetate is a nonsteroidal antiandrogen that selectively binds to the androgen receptor, exerting antiandrogenic activity. This compound has been demonstrated to reduce inflammatory papules and pustules in various animal models. It serves as a valuable reagent for research into conditions driven by androgenic activity, including acne and other androgen-related disorders.

ONC1-13B is a potent antagonist of the androgen receptor (AR), effectively inhibiting PSA expression in prostate cancer cells. This compound markedly reduces prostate cancer cell proliferation in the presence of dihydrotestosterone (DHT) stimulation. ONC1-13B exerts its anti-tumor effects by preventing androgen binding to AR and inhibiting its nuclear translocation, making it a valuable tool for prostate cancer research.

Trestolone acetate is a synthetic anabolic androgenic steroid that primarily targets androgen receptors. It exhibits strong anabolic activity, promoting muscle growth and strength enhancements. This compound is commonly utilized in research focused on hormone regulation, anabolic processes, and potential therapeutic applications in conditions associated with muscle wasting and hormonal imbalances.

Mebolazine is an androgen receptor agonist that exhibits both androgenic and anabolic properties. Its binding to the androgen receptor facilitates the modulation of gene expression associated with muscle growth and development. This compound is commonly utilized in research settings to investigate the physiological effects of androgens and their role in anabolic processes.

Silandrone is a synthetic anabolic-androgenic steroid (AAS) that functions primarily as an androgen receptor modulator. It exhibits significant anabolic activity, promoting muscle growth and strength gains while also exhibiting properties that can help mitigate muscle wasting. Silandrone is utilized in research applications related to androgen receptor signaling, performance enhancement, and muscle physiology studies.

Topterone is an androgen receptor antagonist that specifically inhibits the action of androgens. It demonstrates potent antiandrogenic activity, making it valuable for research focused on androgen-related conditions. This compound is primarily utilized in studies investigating skin conditions and hormonal therapies.

Carbazole derivative 1 is an androgen receptor inhibitor that effectively reduces androgen and estrogen levels in mammals, including humans. This compound demonstrates significant potential in research applications focusing on hormone-related disorders and cancer treatments involving hormonal regulation. Its unique mechanism may provide insights into therapeutic strategies for managing conditions influenced by androgen and estrogen signaling pathways.

UT-34 is a selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader. It exhibits potent inhibition with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR and variants F876L-AR and W741L-AR, respectively. By binding to the ligand-binding domain and the functional AF-1 domain of AR, UT-34 employs the ubiquitin-proteasome pathway to facilitate AR degradation. This compound demonstrates promising anti-prostate cancer activity, making it valuable for research in androgen signaling and cancer therapeutics.

Cyproterone is an antiandrogen that functions by blocking androgen receptors, thereby inhibiting the actions of testosterone. It is primarily utilized in research investigating hypersexuality and prostate cancer, offering insights into hormonal regulation and therapeutic approaches to these conditions. Cyproterone serves as a valuable tool in studying androgen-mediated pathways and their implications in various diseases.

Androgen Receptor Allosteric Antagonist 1 is a competitive allosteric inhibitor of the androgen receptor, exhibiting a Ki of 9 μM. This compound effectively inhibits R1881-mediated transcriptional activity and cell proliferation, making it a valuable tool for studying prostate cancer. Its unique mechanism of action allows for detailed exploration of androgen receptor signaling pathways in cancer research.

CP8754 is a selective antagonist of the human progesterone receptor (hPR), acting primarily by competitively inhibiting the binding of [3H]-progesterone. This compound effectively impedes progesterone-mediated signaling, as evidenced by its ability to inhibit both exogenous luciferase and endogenous alkaline phosphatase expression in vitro, and to suppress rabbit endometrial transformation in vivo. CP8754 exhibits minimal binding affinity for human glucocorticoid receptors, estrogen receptors, and rat androgen receptors, making it a valuable tool for investigating progesterone-related diseases, including breast cancer, endometriosis, uterine fibroids, and hormone-dependent tumors.

17β-Acetoxy-2α-bromo-5α-androstan-3-one is a biochemical assay reagent that functions as a steroid derivative. This compound exhibits significant biological activity as a selective androgen receptor modulator, making it useful for research focused on steroid hormone signaling and metabolic processes. It is valuable for studies investigating androgen-related disorders and the mechanistic pathways influenced by androgens in various biological systems.

Enzalutamide impurity 4 is a recognized impurity associated with Enzalutamide, a potent androgen receptor inhibitor. This compound is essential for analytical research, particularly in assessing the purity and stability of Enzalutamide formulations. It serves as a valuable tool in drug development and quality control processes, facilitating the identification and quantification of impurities in pharmaceutical applications.

(3β,5α)-Androstan-3-amine hydrochloride is a synthetic derivative of the steroid hormone androstenedione, targeting androgen receptors. This compound exhibits significant biological activity, facilitating research in hormonal studies and androgenic activity. It is particularly relevant for investigating steroid signaling pathways and may have applications in drug discovery and development related to androgen-mediated physiological processes.

2α-Methyl androsterone is an anabolic androgenic steroid that acts as a metabolite of mesterolone and drostanolone. It exhibits key biological activities related to androgen receptors, playing a significant role in various androgen-dependent processes. This compound is primarily utilized in research applications focused on steroid hormone metabolism and the development of anabolic therapies.

BWA-522 intermediate-3 is a key intermediate in the synthesis of BWA-522, a small molecule protein-targeting chimera (PROTAC). This compound exhibits potent degradation of androgen receptor full-length (AR-FL) and its variant AR-V7. BWA-522 is primarily used in research applications focusing on hormone-resistant prostate cancer and mechanisms of selective protein degradation.

AH3960 is a selective agonist of the parathyroid hormone receptor 1 (PTHR1). It has demonstrated significant biological activity through its ability to activate PTHR1, contributing to studies in bone metabolism and calcium homeostasis. Additionally, AH3960 exhibits inhibitory effects on androgen receptors, specifically targeting both wild-type and the T877 mutant variant, with an IC50 value of 0.82 μM. This dual functionality makes AH3960 a valuable tool for research in endocrine signaling and related pathways.

Dehydroisoandrosterone 3-acetate is an androgen receptor agonist that serves as a key precursor to testosterone and estrogen. It plays a significant role in modulating vertebrate aggression and has been utilized in research to explore its effects on hormonal pathways and behavioral responses. This compound is particularly useful for studies investigating androgenic activity and its implications in various physiological and psychological processes.

11β,17β-Dihydroxy-5α-androstan-3-one is a C11-oxy C19 steroid that functions as a potent androgen. This compound exhibits significant biological activity in androgen receptor modulation, making it an important tool for exploring prostate cancer mechanisms. Researchers can utilize 11OHDHT to investigate its effects on androgen signaling pathways and develop potential therapeutic strategies in prostate cancer treatment.

p,p'-DDE (4,4'-DDE) serves as a potent androgen receptor antagonist, exhibiting an IC50 value of 5 μM and a Ki of 3.5 μM. This compound plays a significant role in the disruption of male reproductive system development and function. Furthermore, elevated levels of p,p'-DDE in serum have been associated with an increased risk of type 2 diabetes in women, highlighting its relevance in endocrine disruption studies and metabolic research.