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-B1986R
    p,p'-DDE (Standard)
    		Antagonist
    p,p'-DDE (Standard) is the analytical standard of p,p'-DDE. This product is intended for research and analytical applications. p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
    p,p'-DDE (Standard)
  • HY-16060R
    Apalutamide (Standard)
    		Antagonist
    Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide (Standard)
  • HY-B2044
    Bromopropylate
    		Inhibitor
    Bromopropylate is a pesticide with moderate anti-androgenic activities.
    Bromopropylate
  • HY-B1866R
    Linuron (Standard)
    		Antagonist
    Linuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
    Linuron (Standard)
  • HY-W753141
    p,p'-DDE-13C12
    		Antagonist
    p,p'-DDE-13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM.
    p,p'-DDE-<sup>13</sup>C<sub>12</sub>
  • HY-N0475R
    Triptophenolide (Standard)
    		Antagonist
    Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer.
    Triptophenolide (Standard)
  • HY-107480R
    YK11 (Standard)
    		Agonist
    YK11 (Standard) is the analytical standard of YK11. This product is intended for research and analytical applications. YK11 is a partial agonist of androgen receptor, with osteogenic activity.
    YK11 (Standard)
  • HY-164477
    FL442
    		Modulator
    FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL).
    FL442
  • HY-B1234S
    Octinoxate-13C,d3
    		Modulator
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate-<sup>13</sup>C,d<sub>3</sub>
  • HY-15194R
    Dimethylcurcumin (Standard)
    		Inhibitor
    Dimethylcurcumin (Standard) is the analytical standard of Dimethylcurcumin. This product is intended for research and analytical applications. Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
    Dimethylcurcumin (Standard)
  • HY-14249R
    Bicalutamide (Standard)
    		Antagonist
    Bicalutamide (Standard) is the analytical standard of Bicalutamide. This product is intended for research and analytical applications. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide (Standard)
  • HY-105318R
    LGD-2226 (Standard)
    		Modulator
    LGD-2226 (Standard) is the analytical standard of LGD-2226 (HY-105318). This product is intended for research and analytical applications. LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.
    LGD-2226 (Standard)
  • HY-13331S1
    Clascoterone-d6
    		Antagonist
    Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
    Clascoterone-d<sub>6</sub>
  • HY-176129
    AR ligand 41
    		Ligand
    AR ligand 41 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). AR ligand 41 can be used for the synthesis of BWA-6047 (HY-176128).
    AR ligand 41
  • HY-109070R
    Ralaniten (Standard)
    		Antagonist
    Ralaniten (Standard) is the analytical standard of Ralaniten (HY-109070). This product is intended for research and analytical applications. Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
    Ralaniten (Standard)
  • HY-114744
    6α-Hydroxy metandienone
    6α-Hydroxy metandienone is an androgenic anabolic steroid metabolite of Metandienone.
    6α-Hydroxy metandienone
  • HY-B1234A
    (E)-Octinoxate
    		Inhibitor 98.79%
    (E)-Octinoxate is the isomer of Octinoxate (HY-B1234). Octinoxate 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.
    (E)-Octinoxate
  • HY-131953
    Androgen receptor-IN-3
    		Inhibitor
    Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM.
    Androgen receptor-IN-3
  • HY-13702R
    Nilutamide (Standard)
    		Antagonist
    Nilutamide (Standard) is the analytical standard of Nilutamide. This product is intended for research and analytical applications. Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties.
    Nilutamide (Standard)
  • HY-13331R
    Clascoterone (Standard)
    		Antagonist
    Clascoterone (Standard) is the analytical standard of Clascoterone. This product is intended for research and analytical applications. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
    Clascoterone (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity