2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor

Androgen Receptor

Androgen Receptor

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Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0561S4
    Spironolactone-d6-1
    		99.26%
    Spironolactone-d6-1 is the deuterium labeled Spironolactone (HY-B0561). Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca2+ channels to exert antihypertensive effects.
    Spironolactone-d<sub>6</sub>-1
  • HY-116214R
    Cyprodinil (Standard)
    		Agonist
    Cyprodinil (Standard) (CGA-219417 (Standard)) is the analytical standard of Cyprodinil (HY-116214). This product is intended for research and analytical applications. Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil (Standard)
  • HY-170820
    XYD049
    		Inhibitor 99.46%
    XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822).
    XYD049
  • HY-111803
    4'-Methoxyflavonol
    		Inhibitor 98.00%
    4'-Methoxyflavonol is a flavonol. 4'-Methoxyflavonol reduces androgen receptor and increases SOD. 4'-Methoxyflavonol reduces plasma glucose, cholesterol, and triglycerides. 4'-Methoxyflavonol has anti-stress and antioxidant activities. 4'-Methoxyflavonol can be used in prostate cancer research.
    4'-Methoxyflavonol
  • HY-70002BS
    Enzalutamide carboxylic acid-d6
    		98.99%
    Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide.
    Enzalutamide carboxylic acid-d<sub>6</sub>
  • HY-13273S
    Ostarine-d4
    		Modulator 99.9%
    Ostarine-d4 is a deuterated labeled Ostarine.
    Ostarine-d<sub>4</sub>
  • HY-45509
    TLB 150 Benzoate
    		Modulator 98.3%
    TLB 150 Benzoate (RAD150) is a nonsteroidal androgen receptor modulator with an IC50 value of 0.13 μM. TLB 150 Benzoate spontaneously cyclizes under physiological conditions to form RAD 179, resulting in a persistent, reversible, and slow neuronal conduction blockade. TLB 150 Benzoate can be used for research on neurological diseases.
    TLB 150 Benzoate
  • HY-171048
    GTx-027
    		Modulator 99.61%
    GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI).
    GTx-027
  • HY-111145
    RD162
    		Antagonist 99.69%
    RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
    RD162
  • HY-B0022R
    Flutamide (Standard)
    		Antagonist
    Flutamide (Standard) is the analytical standard of Flutamide. This product is intended for research and analytical applications. Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.
    Flutamide (Standard)
  • HY-N0790R
    Lupeol (Standard)
    		Inhibitor
    Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
    Lupeol (Standard)
  • HY-W653723
    N-Nitrosodicyclohexylamine
    		Antagonist 99.0%
    N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein.
    N-Nitrosodicyclohexylamine
  • HY-16060S2
    Apalutamide-13C,d3
    		Antagonist 99.90%
    Apalutamide-13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-<sup>13</sup>C,d<sub>3</sub>
  • HY-N16483
    Procyanidin B2-3'-O-gallate
    		Inhibitor
    Procyanidin B2-3'-O-gallate is a mono-gallate ester that can be found in grape seed extract. Procyanidin B2-3'-O-gallate induces cleavage of caspase-9, caspase-3, and PARP, reduces levels of Bcl-2, Bcl-Xl, and androgen receptor and induces apoptosis. Procyanidin B2-3'-O-gallate can be used for the research of prostate cancer.
    Procyanidin B2-3'-O-gallate
  • HY-B1978R
    Iprodione (Standard)
    		Inhibitor
    Iprodione (Standard) is the analytical standard of Iprodione. This product is intended for research and analytical applications. Iprodione is an orally active diformimide fungicide. Iprodione can specifically cause oxidative damage by producing free radicals (ROS). Iprodione is also an antiandrogen agent that delays adolescent development in rats and reduces sexual behavior and reproductive ability in rats.
    Iprodione (Standard)
  • HY-U00229
    Bifluranol
    		Inhibitor 98.88%
    Bifluranol (BX341) is an anti-androgen.
    Bifluranol
  • HY-138089
    17β-Hydroxy exemestane
    		Agonist 98.21%
    17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
    17β-Hydroxy exemestane
  • HY-16985R
    Darolutamide (Standard)
    		Antagonist
    Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer.
    Darolutamide (Standard)
  • HY-B1234R
    Octinoxate (Standard)
    		Modulator
    Octinoxate (Standard) is the analytical standard of Octinoxate. This product is intended for research and analytical applications. Octinoxate (Octyl methoxycinnamate) is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage and can be used to reduce the appearance of scars. Octinoxate also has a complex androgenic and estrogenic effect.
    Octinoxate (Standard)
  • HY-13604R
    Cyproterone acetate (Standard)
    		Antagonist
    Cyproterone acetate (Standard) is the analytical standard of Cyproterone acetate. This product is intended for research and analytical applications. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.
    Cyproterone acetate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity